674 articles for thisTarget
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The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A
Universita Degli Studi Di Firenze
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
Advinus Therapeutics
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
Advinus Therapeutics
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent A
Universita Degli Studi Di Firenze
Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A
Leiden University
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Discovery of 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine derivatives as novel adenosine A
North-West University
Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.
RhôNe-Poulenc Rorer
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of 7-(Prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A2A Adenosine Receptor: Prediction from Molecular Modeling.
Julius-Maximilians-Universit£T W£Rzburg
Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.
Jagiellonian University Medical College
Exploring the 2- and 5-positions of the pyrazolo[4,3-d]pyrimidin-7-amino scaffold to target human A1 and A2A adenosine receptors.
Universita Degli Studi Di Firenze
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.
Uppsala University
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Astrazeneca
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.
University of Warwick
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.
Georgia Institute of Technology
Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists.
North-West University
Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.
Merck Research Laboratories
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor.
Universita Degli Studi Di Firenze
5,7-Disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazines as pharmacological tools to explore the antagonist selectivity profiles toward adenosine receptors.
University of Trieste
1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor.
North-West University
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
Leiden University
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study.
University of Ferrara
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.
Merck Research Laboratories
One-pot reaction to obtain N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold as human A3 adenosine receptor antagonists.
University of Ferrara
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors.
University of Barcelona
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.
University of Ferrara
5'-C-Ethyl-tetrazolyl-N(6)-substituted adenosine and 2-chloro-adenosine derivatives as highly potent dual acting A1 adenosine receptor agonists and A3 adenosine receptor antagonists.
University of Camerino
A facile and novel synthesis of N(2)-, C(6)-substituted pyrazolo[3,4-d]pyrimidine-4 carboxylate derivatives as adenosine receptor antagonists.
National University of Singapore
Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.
H. Lundbeck
Novel thiazole-thiophene conjugates as adenosine receptor antagonists: synthesis, biological evaluation and docking studies.
B. V. Patel Pharmaceutical Education and Research Development (Perd) Centre
7-Amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives: structural investigations at the 5-position to target human A1 and A(2A) adenosine receptors. Molecular modeling and pharmacological studies.
University of Florence
Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study.
University of Trieste
Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
1,2,4-triazolo[1,5-a]quinoxaline derivatives and their simplified analogues as adenosine A3 receptor antagonists. Synthesis, structure-affinity relationships and molecular modeling studies.
University of Florence
Further studies on pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective human A1 adenosine receptor antagonists.
Universita Degli Studi Di Firenze
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.
University of Ferrara
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Astrazeneca
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.
Leiden University
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model.
National Institute of Diabetes
De-novo designed library of benzoylureas as inhibitors of BCL-XL: synthesis, structural and biochemical characterization.
The Walter and Eliza Hall Institute of Medical Research
Fluorescent ligands for adenosine receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.
National Institute of Diabetes and Digestive and Kidney Diseases
Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1).
Astrazeneca
2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and selective human A3 adenosine receptor antagonists. Molecular modeling studies and pharmacological evaluation.
University of Florence
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.
University of Bonn
Selective and potent adenosine A3 receptor antagonists by methoxyaryl substitution on the N-(2,6-diarylpyrimidin-4-yl)acetamide scaffold.
University of Santiago De Compostela
Pyrazolo[1,5-c]quinazoline derivatives and their simplified analogues as adenosine receptor antagonists: synthesis, structure-affinity relationships and molecular modeling studies.
Universita' Di Firenze
Highly potent and selective fluorescent antagonists of the human adenosine A3 receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.
University of Nottingham
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.
University of Nottingham
A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor.
Center For Bio-Pharmaceutical Sciences
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.
TBA
Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists.
Universidade De A Coru£A
In silico directed chemical probing of the adenosine receptor family.
Universidade Do Minho
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists.
Universidade De Porto
Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfuryl xanthines as adenosine receptor antagonists.
Universidade De Santiago De Compostela
Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists.
Universidade De A Coru£A
QSAR study on a novel series of 8-azaadenine analogues proposed as A1 adenosine receptor antagonists.
University of Pisa
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
University of Bari Aldo Moro
2-aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
University of South Florida
Exploring the directionality of 5-substitutions in a new series of 5-alkylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine as a strategy to design novel human a(3) adenosine receptor antagonists.
University of Trieste
Medicinal chemistry of A3 adenosine receptor modulators: pharmacological activities and therapeutic implications.
University of Ferrara
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor.
University of Ferrara
Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data.
Leiden/Amsterdam Center For Drug Research
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.
University of North Carolina At Chapel Hill
Design and characterization of optimized adenosine A2A/A1 receptor antagonists for the treatment of Parkinson's disease.
Janssen Research and Development
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.
Jagiellonian University Medical College
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.
TBA
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists.
University of Ferrara
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
National Institute of Diabetes and Digestive and Kidney Diseases
New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.
Universidade Do Minho
Synthesis and pharmacological evaluation of dual acting antioxidant A(2A) adenosine receptor agonists.
Monash University
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.
TBA
Exploring activity cliffs in medicinal chemistry.
Rheinische Friedrich-Wilhelms-Universit£T
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A2B adenosine receptor antagonists.
University of Pisa
Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.
Heptares Therapeutics
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
TBA
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.
H. Lundbeck
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
Freie Universit£T Berlin
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Roche Research Center
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
University of Pisa
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
University of Delhi
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
University of Bonn
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Institute
High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.
University of Bonn
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
University of Camerino
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.
Leiden University
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S of Maine
Synthesis of eudistomin D analogues and its effects on adenosine receptors.
Hokkaido University
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
Vernalis (R&D)
Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Vernalis (R&D)
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.
Vernalis (R&D)
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
Cv Therapeutics
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.
University of Ferrara
N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.
Monash University (Parkville Campus)
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Leiden/Amsterdam Center For Drug Research
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
University of Bari Aldo Moro
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Ewha Womans University
New QSAR combined strategy for the design of A1 adenosine receptor agonists.
Central University of Las Villas
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
University of Camerino
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.
Novartis Institutes of Biomedical Research
Structure-activity relationships of adenosines with heterocyclic N6-substituents.
Monash University (Parkville Campus)
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
University of Pisa
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.
University of Ferrara
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
Biogen Idec
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
University of Camerino
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.
University of Ferrara
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Pfizer
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
University of California San Francisco
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.
University of Virginia
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
University of Trieste
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
University of Naples Federico II
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
University of Urbino
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.
University of Ferrara
Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Biogen Idec
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
University of Camerino
6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency.
University of Virginia
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
University of Ferrara
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
Cv Therapeutics
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
Iiqab (Csic)
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Novartis Institutes For Biomedical Research
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists.
Experimental Sugar Cane Station
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.
Ewha Womans University
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
University of Bonn
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
University of Ferrara
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
University of Leiden
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
Universita Degli Studi Di Firenze
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.
Universitat Pompeu Fabra
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Leiden University
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
University of Ferrara
Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
University of Camerino
Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.
University of Genoa
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Leiden/Amsterdam Center For Drug Research
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
University of Bonn
N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
University of Camerino
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
Vrije Universiteit
Design, synthesis, and evaluation of novel A2A adenosine receptor agonists.
University of Virginia
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
University of Pisa
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
National Institute of Diabetes and Digestive and Kidney Diseases
Nucleosides and nucleotides. 200. Reinvestigation of 5'-N-ethylcarboxamidoadenosine derivatives: structure-activity relationships for P(3) purinoceptor-like proteins.
Hokkaido University
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
Leiden/Amsterdam Center For Drug Research
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
University of Camerino
A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.
University of Pisa
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
National Institute of Diabetes
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
Leiden/Amsterdam Center For Drug Research
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Leiden University
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.
University of Ferrara
Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.
Hokkaido University
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
University of Camerino
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.
University of Ghent
N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors.
Leiden/Amsterdam Center For Drug Research
Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors.
University of Ferrara
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes
2-alkenyl and 2-alkyl derivatives of adenosine and adenosine-5'-N-ethyluronamide: different affinity and selectivity of E- and Z-diastereomers at A2A adenosine receptors.
University of Camerino
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
National Institute of Diabetes
2-Aralkynyl and 2-heteroalkynyl derivatives of adenosine-5'-N-ethyluronamide as selective A2a adenosine receptor agonists.
University of Camerino
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
National Institute of Diabetes
Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor.
Leiden University
2-[N'-(3-arylallylidene)hydrazino]adenosines showing A2a adenosine agonist properties and vasodilation activity.
University of Milan
Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
National Institute of Diabetes
N6-substituted adenosine receptor agonists. Synthesis and pharmacological activity as potent antinociceptive agents.
Carpibem
Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives.
National Institute of Diabetes
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
National Institute of Diabetes
2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation.
University of Camerino
Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine.
Kyowa Hakko Kogyo
Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
Kyowa Hakko Kogyo
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Kyowa Hakko Kogyo
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
Niddk
2-(N'-aralkylidenehydrazino)adenosines: potent and selective coronary vasodilators.
University of South Florida
Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.
National Institute of Diabetes
Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects.
Hokkaido University
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
Kyowa Hakko Kogyo
Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity.
Hokkaido University
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.
University of Camerino
Nucleosides and nucleotides. 107. 2-(cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects.
Yamasa Shoyu
N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.
University of South Florida
Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines.
Ciba-Geigy
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
University of South Florida
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Center For Bio-Pharmaceutical Sciences
N6-substituted adenosine receptor agonists: potential antihypertensive agents.
Warner-Lambert
Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.
University of South Florida
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
Pfizer
2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands.
Ciba-Geigy
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
Merrell Dow Research Institute
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
Niddk
C2,N6-disubstituted adenosines: synthesis and structure-activity relationships.
Warner-Lambert
Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.
Niddk
N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
Warner-Lambert
N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.
Warner-Lambert
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
University of Camerino
Photoaffinity labeling adenosine A1 receptors with an antagonist 125I-labeled aryl azide derivative of 8-phenylxanthine.
University of Virginia School of Medicine
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
University of Virginia School of Medicine
N6-(arylalkyl)adenosines. Identification of N6-(9-fluorenylmethyl)adenosine as a highly potent agonist for the adenosine A2 receptor.
Warner-Lambert
N6-phenyladenosines: pronounced effect of phenyl substituents on affinity for A2 adenosine receptors.
TBA
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
Parke-Davis Pharmaceutical Research Division
N6-substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors.
TBA
Functionalized congeners of adenosine: preparation of analogues with high affinity for A1-adenosine receptors.
TBA
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
TBA
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
TBA
Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.
Cv Therapeutics
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.
Seoul National University
Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
Vrije Universiteit
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
University of Pisa
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
University of Camerino
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Niddk
The discovery and synthesis of highly potent, A2a receptor agonists.
Glaxowellcome Medicines Research Centre
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.
University of Amsterdam
Diimidazo[1,2-c:4',5'-e]pyrimidines: N6-N1 conformationally restricted adenosines.
Griffith University
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.
Griffith University
Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives.
Glaxowellcome Medicines Research Center
New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
TBA
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A2B adenosine receptor antagonists.
University of Ferrara
Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A2A adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A2A and A3 adenosine receptor ligands.
Ewha Womans University
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
University of Ferrara
Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1-yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A¿? adenosine receptor.
University of Ferrara
Synthesis and Biological Evaluation of a New Series of 1,2,4-Triazolo[1,5-a]-1,3,5-triazines as Human A(2A) Adenosine Receptor Antagonists with Improved Water Solubility.
Universita Di Trieste
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
Pfizer
Does the combination of optimal substitutions at the C²-, N¿?¿- and N¿?¿-positions of the pyrazolo-triazolo-pyrimidine scaffold guarantee selective modulation of the human A3 adenosine receptors?
National University of Singapore
New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists.
University of Ferrara
Synthesis, structure-affinity relationships, and molecular modeling studies of novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Universita' Di Firenze
Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.
National Institute of Diabetes and Digestive and Kidney Diseases
The identification of the 2-phenylphthalazin-1(2H)-one scaffold as a new decorable core skeleton for the design of potent and selective human A3 adenosine receptor antagonists.
Universita` Degli Studi Di Firenze
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.
Roche Research Center
Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection.
Pfizer
Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist
TBA
Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists.
University of Santiago De Compostela
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.
Johnson & Johnson Pharmaceutical Research and Development
Molecular modeling study on potent and selective adenosine A(3) receptor agonists.
University of Camerino
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Dipartimento Di Scienze Farmaceutiche
Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists.
Bayer Schering Pharma
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.
Ewha Womans University
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.
H. Lundbeck
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
East China University of Science and Technology
Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.
Monash University
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine receptor ligands.
Institute of Chemical Technology
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA(3) adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition.
National University of Singapore
Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.
National University of Singapore
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement.
RhôNe-Poulenc Rorer
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
RhôNe-Poulenc Rorer
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Novartis Institutes For Biomedical Research
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.
Universidad De M£Laga
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Ewha Womans University
3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists.
Monash University (Parkville Campus)
Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase.
University of Bonn
2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition.
University of Florence
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor.
University of Camerino
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.
Aix-Marseille Universit£
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
University of Padova
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors.
Hokkaido University
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Ewha Womans University
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.
Vernalis (R+D)
Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.
University of Antwerp
Synthesis of 5-(3-Hydroxypropyl)-7-methoxy-2-(3‘-methoxy-4‘-hydroxyphenyl)-3- benzo[b]furancarbaldehyde, a Novel Adenosine A1 Receptor Ligand from the Root of Salvia miltiorrhiza
TBA
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
TBA
Synthesis of new pyrazolo[4,3-e]1,2,4-triazolo[1,5-c] pyrimidine and 1,2,3-triazolo[4,5-e]1,2,4-triazolo[1,5-c] pyrimidine displaying potent and selective activity as A2a adenosine receptor antagonists.
TBA
The synthesis and biochemical evaluation of new A1 selective adenosine receptor agonists containing 6-hydrazinopurine moieties
TBA
A note of caution in the use of receptor binding assays to screen marine organisms: the action of halistanol trisulphate on adenosine receptors.
TBA
An explanation of the substituent effect of 1,3,8-trisubstituted xanthines on adenosine A1/A2 affinity.
TBA
1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.
Universidade De Santiago De Compostela
N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
University of Camerino
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Universita Di Firenze
Synthesis, biological assays and QSAR studies of N-(9-benzyl-2-phenyl-8-azapurin-6-yl)-amides as ligands for A1 adenosine receptors.
Università
Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists.
Pharmacopeia
N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Neurocrine Biosciences
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
Vernalis R&D
Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists.
Pharmacopeia
Synthesis of a series of 8-(substituted-phenyl)xanthines and a study on the effects of substitution pattern of phenyl substituents on affinity for adenosine A(1) and A(2A) receptors.
University Institute of Pharmaceutical Sciences
Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists.
Università
Novel potent and highly selective human A(3) adenosine receptor antagonists belonging to the 4-amido-2-arylpyrazolo[3,4-c]quinoline series: molecular docking analysis and pharmacological studies.
Università
1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.
Università
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Neurocrine Biosciences
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Ewha Womans University
2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.
Monash University
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.
Dipartimento Di Scienze Farmaceutiche
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Universita' Di Firenze
N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.
Università
Synthesis and adenosine receptor binding studies of some novel triazolothienopyrimidines.
University College of Pharmaceutical Sciences
Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.
University of Bonn
Naturally occurring cembranes from an Australian sarcophyton species.
Astrazeneca R&D Griffith University
Isolation of psammaplin A 11'-sulfate and bisaprasin 11'-sulfate from the marine sponge Aplysinella rhax.
Griffith University
Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.
Griffith University
Isolation of xestosterol esters of brominated acetylenic fatty acids from the marine sponge xestospongia testudinaria
Griffith University
Interference of linoleic acid fraction in some receptor binding assays.
Leiden University
Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp.
Institut FüR Biowissenschaften
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Neurocrine Biosciences
Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines.
Cv Therapeutics
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Neurocrine Biosciences
Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.
Jagiellonian University Medical College
Dual acting antioxidant A1 adenosine receptor agonists.
Monash University (Parkville Campus)
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Università
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.
Santaris Pharma
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
Ewha Womans University
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.
Institut D'Investigacions BiomèDiques August Pi I
N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.
Jagiellonian University
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A
Seoul National University
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Almirall
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.
Insilico Medicine Hong Kong
Structure-based virtual screening discovers potent and selective adenosine A
Uppsala University
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Exploring the Effect of Halogenation in a Series of Potent and Selective A
University of Santiago de Compostela
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
Schering-Plough Research Institute
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Ghent University
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.
Biogen Idec
Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Biogen Idec
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.
Cv Therapeutics
Synthesis, biological activity and molecular modelling of new trisubstituted 8-azaadenines with high affinity for A1 adenosine receptors.
Università
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches.
Vernalis (R&D)
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
University of Bonn
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.
Università
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Università
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
Cv Therapeutics
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Leiden University
New pyrrolopyrimidin-6-yl benzenesulfonamides: potent A2B adenosine receptor antagonists.
RhôNe-Poulenc Rorer
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Ewha Womans University
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
National Institute of Diabetes and Digestive and Kidney Diseases
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Università
Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer.
Università
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors.
Università
Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.
Cv Therapeutics
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists.
Biogen Idec
1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors.
Dipartimento Di Scienze Farmaceutiche
New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists.
Università
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
New pyrrolo[2,1-f]purine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives as potent and selective human A3 adenosine receptor antagonists.
Università
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A
University of Southern California
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
University of Dundee
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
Zhejiang University
Adenosine receptor antagonists: Recent advances and therapeutic perspective.
Isf College of Pharmacy
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.
National and Kapodistrian University of Athens
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
Cv Therapeutics
Synthesis of alkyne derivatives of a novel triazolopyrazine as A(2A) adenosine receptor antagonists.
Biogen Idec
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A
University of Bern
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A
Universidade De Santiago De Compostela
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A
Monash University
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
Biogen Idec
Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
Biogen Idec
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Biogen Idec
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A
Leiden University
Exploring Non-orthosteric Interactions with a Series of Potent and Selective A
Universidade De Santiago De Compostela
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Otsuka Pharmaceutical Factory
A mild, efficient and alpha-selective glycosidation by using potassium dodecatungstocobaltate trihydrate as catalyst.
University of Isfahan
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A
Shanghaitech University
Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A
Ewha Womans University
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
Università
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
F. Hoffmann-La Roche
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Janssen Research & Development
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Inotek Pharmaceuticals
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
University of Bonn
Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.
F. Hoffmann-La Roche
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.
Leiden University
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).
Cv Therapeutics
Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: Towards adenosine A
Sun Yat-Sen University
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as adenosine receptor antagonists. Influence of the N5 substituent on the affinity at the human A 3 and A 2B adenosine receptor subtypes: a molecular modeling investigation.
Università
2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications.
Deakin University
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
University of Cologne
Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A
National Institute of Diabetes and Digestive and Kidney Disease
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.
Pfizer
Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging.
Forschungszentrum JüLich
Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists.
Università
New irreversible adenosine A(1) antagonists based on FSCPX.
Monash University (Parkville Campus)
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.
Cv Therapeutics
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.
Nutrition Research Institute
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.
TBA
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Instituto De QuíMica MéDica (Csic)
2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.
University of Virginia
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
National Institute of Diabetes & Digestive & Kidney Diseases
Biological Evaluation of 5'-(
National Institute of Diabetes and Digestive and Kidney Diseases
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
Ghent University
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.
St. John'S University
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
University of Bonn
Substituted 4-phenylthiazoles: Development of potent and selective A
University of Bonn
Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A(3) adenosine receptor antagonists.
Università
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
Università
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.
Taipei Medical University
Synthesis and biological data of 4-amino-1-(2-chloro-2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl esters, a new series of A1-adenosine receptor (A1AR) ligands.
Facoltà
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.
Niddk
New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A
Universita Degli Studi Di Firenze
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A
Universita Degli Studi Di Firenze
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.
Università
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Leiden/Amsterdam Center For Drug Research
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A
Uppsala University
High-pressure synthesis of enantiomerically pure C-6 substituted pyrazol.
Astrazeneca R&D Griffith University
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Eisai
Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A(1)-adenosine receptor.
Deakin University
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.
Università
7-Deazaadenines bearing polar substituents: structure-activity relationships of new A(1) and A(3) adenosine receptor antagonists.
University of Leipzig
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.
University of Milano-Bicocca
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
Jagiellonian University Medical College
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Universita' Di Firenze
8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors.
University of Bonn
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Vrije Universiteit
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
National Institute of Diabetes
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.
Universita' Di Firenze
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.
Università
Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.
University of WüRzburg
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.
Universita Degli Studi Di Firenze
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College of Wisconsin
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Università
Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.
National Institute of Diabetes
Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.
Leiden/Amsterdam Center For Drug Research
N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
Novo Nordisk
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.
Cadus Pharmaceutical
Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.
Fujisawa Pharmaceutical
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
National Institute of Diabetes
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A
Leiden University
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.
Novo Nordisk
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A
National Engineering Research Center For The Emergency Drug
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Vrije Universiteit
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Vrije Universiteit
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
National Institute of Diabetes
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.
University of Science & Technology (Ust)
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
Università
Novel 3-aralkyl-7-(amino-substituted)-1,2,3-triazolo[4,5-d]pyrimidines with high affinity toward A1 adenosine receptors.
Università
A1 adenosine receptor antagonists as ligands for positron emission tomography (PET) and single-photon emission tomography (SPET).
Forschungszentrum JüLich
Synthesis and structure-activity relationships of 3,7-dimethyl-1-propargylxanthine derivatives, A2A-selective adenosine receptor antagonists.
Julius-Maximilians-UniversitäT WüRzburg
Novel human adenosine receptor antagonists based on the 7-amino-thiazolo[5,4-d]pyrimidine scaffold. Structural investigations at the 2-, 5- and 7-positions to enhance affinity and tune selectivity.
Universita Degli Studi Di Firenze
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Cv Therapeutics
Synthesis and structure-activity relationship of pyrazolo[3,4-d]pyrimidines: potent and selective adenosine A1 receptor antagonists.
Griffith University
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
National Institute of Diabetes
Synthesis and cardiotonic activity of novel pyrimidine derivatives: crystallographic and quantum chemical studies.
Università
Chiral pyrrolo[2,3-d]pyrimidine and pyrimido[4,5-b]indole derivatives: structure-activity relationships of potent, highly stereoselective A1-adenosine receptor antagonists.
Julius-Maximilians-UniversitäT WüRzburg
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
National Institute of Diabetes
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.
Università
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.
Stockholm University
Structure-Based Design, Synthesis by Click Chemistry and
National Institute of Diabetes and Digestive and Kidney Diseases
Interactions of flavonoids and other phytochemicals with adenosine receptors.
National Institute of Diabetes
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
National Institute of Diabetes
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Hokuriku University
Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
National Institute of Diabetes
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
National Institutes of Health
Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists.
Seoul National University
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity.
Panjab University
Xanthines with C8 chiral substituents as potent and selective adenosine A1 antagonists.
Marion Merrell Dow Research Institute
Discovery of simplified N²-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: efficient synthetic approaches, biological evaluations and molecular docking studies.
National University of Singapore
Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Pharmazeutische Chemie
Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor.
University of Ferrara
Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
Eberhard-Karls-UniversitäT TüBingen
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.
University of Bonn
Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.
University of Santiago De Compostela
8-(2-Furyl)adenine derivatives as A₂A adenosine receptor ligands.
University of Camerino
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Smithkline Beecham Pharmaceuticals
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.
University of Pisa
Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors.
University of South Florida
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
University of Delhi
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
University of Urbino
New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides.
B.V. Patel Pharmaceutical Education and Research Development
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.
University of Bonn
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.
Monash University (Parkville Campus)
Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.
Janssen Research & Development
Tricyclic heteroaromatic systems. Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines.
Università
Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2'-furyl)-1,2,4-triazolo[1,5-a]quinoxalines.
University of Santiago De Compostela
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
Leiden/Amsterdam Center For Drug Research
Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.
Fujisawa Pharmaceutical
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A
University of Trieste
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
TBA
Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors.
TBA
Antagonists of the adenosine A
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer
Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
Ciba-Geigy
[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.
Warner-Lambert
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
Merrell Dow Research Institute
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A
Universita Degli Studi Di Firenze
Analogues of 1,3-dipropyl-8-phenylxanthine: enhancement of selectivity at A1-adenosine receptors by aryl substituents.
TBA
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
TBA
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.
University of Kwazulu-Natal
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
Warner-Lambert
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
TBA
Structure-activity relationship studies and pharmacological characterization of N
Universita Degli Studi Di Firenze
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
University of South Florida
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
National Institutes of Health
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Janssen Infectious Diseases-Diagnostics
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties.
Center For Bio-Pharmaceutical Sciences
Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human A
Universita Degli Studi Di Firenze
Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease.
Uppsala University
7-Deaza-2-phenyladenines: structure-activity relationships of potent A1 selective adenosine receptor antagonists.
National Institute of Diabetes
Imidazodiazepinediones: a new class of adenosine receptor antagonists.
National Institute of Diabetes
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Development of novel pyridazinone-based adenosine receptor ligands.
Universita Degli Studi Di Firenze
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
Nova Pharmaceutical
8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities.
Kyowa Hakko Kogyo
Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine.
Griffith University
Imidazo[1,2-a]pyrazin-8-amine core for the design of new adenosine receptor antagonists: Structural exploration to target the A
Universita Degli Studi Di Firenze
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.
Vanderbilt University
(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.
Kyowa Hakko Kogyo
Conformationally restrained, chiral (phenylisopropyl)amino-substituted pyrazolo[3,4-d]pyrimidines and purines with selectivity for adenosine A1 and A2 receptors.
Marion Merrell Dow Research Institute
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A
University of Camerino
2-(N'-alkylidenehydrazino)adenosines: potent and selective coronary vasodilators.
University of South Florida
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
Kyowa Hakko Kogyo
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Hokuriku University
SALT FORM AND CRYSTAL FORM OF PYRAZOLE SUBSTITUTED IMIDAZO[1,2- A]QUINOXALINE DERIVATIVE
Ocumension Therapeutics (Suzhou) Co.
Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors
Pfizer
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists
Tufts College
Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
Boehringer Ingelheim International
Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
Amgen
1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions
Sabila Biosciences
Benzopiperdine derivatives and their use in the treatment of cancer and hemoglobinopathies
Ctxt
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
Universitetet I Oslo
N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders
Ogeda
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Chemokine CXCR1 and CXCR2 receptor antagonist compounds, and use thereof in the treatment of chemokine-mediated pathologies
Galderma Research & Development
3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
Samumed
Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold.
The University of Kansas
Rationally designed sulfamides as glutamate carboxypeptidase II inhibitors.
Washington State University At Pullman
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme
Altered enthalpy-entropy compensation in picomolar transition state analogues of human purine nucleoside phosphorylase.
Albert Einstein College of Medicine
Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents.
Central Institute of Medicinal and Aromatic Plants
Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed.
University of Copenhagen
M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. I. Normal rat bladder.
Temple University
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.
Kyowa Hakko Kogyo
Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist.
Sanofi-Synthelabo Recherche
Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications.
Biocentre Niederursel
Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
R. W. Johnson Pharmaceutical Research Institute
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences.
Eli Lilly
Molecular cloning and characterization of the human A3 adenosine receptor.
Merck Research Laboratories
Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications.
Maryland Psychiatric Research Center
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.
Northern Kentucky University
Discovery of antibacterial biotin carboxylase inhibitors by virtual screening and fragment-based approaches.
Pfizer
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Takeda Pharmaceutical
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation.
Merck Research Laboratories
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
Csic
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Pfizer
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.
Abbott Laboratories
Discovery of Boronic Acids as Novel and Potent Inhibitors of Fatty Acid Amide Hydrolase.
University of Oxford
Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases.
University of Oxford
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
Astrazeneca
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
Irbm/Merck Research Laboratories
Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Rheinische Friedrich-Wilhelms-Universitat Bonn
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.
Novartis Pharmaceuticals
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
University of Bologna
5-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Glaxosmithkline
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Smithkline Beecham Pharmaceuticals