117 articles for thisTarget
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Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Chrysophaentins are competitive inhibitors of FtsZ and inhibit Z-ring formation in live bacteria.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
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
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
Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.
National Institute of Diabetes and Digestive and Kidney Diseases
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
National Institute of Diabetes and Digestive and Kidney Diseases
Fluorinated phenylcyclopropylamines. 1. Synthesis and effect of fluorine substitution at the cyclopropane ring on inhibition of microbial tyramine oxidase.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclase.
National Institute of Diabetes and Digestive and Kidney Diseases
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
National Institute of Diabetes and Digestive and Kidney Diseases
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid r
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at sigma receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds.
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6 beta-iodo
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity relationship of C5-substituted analogues of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine [(+-)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery and synthesis of namalide reveals a new anabaenopeptin scaffold and peptidase inhibitor.
National Institute of Diabetes and Digestive and Kidney Diseases
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
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
Susceptibility and mode of binding of the Mycobacterium tuberculosis cysteinyl transferase mycothiol ligase to tRNA synthetase inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.
National Institute of Diabetes and Digestive and Kidney Diseases
Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines.
National Institute of Diabetes and Digestive and Kidney Diseases
Molecular recognition in the P2Y(14) receptor: Probing the structurally permissive terminal sugar moiety of uridine-5'-diphosphoglucose.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
National Institute of Diabetes and Digestive and Kidney Diseases
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
Natural products, small molecules, and genetics in tuberculosis drug development.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis of natural product-inspired inhibitors of Mycobacterium tuberculosis mycothiol-associated enzymes: the first inhibitors of GlcNAc-Ins deacetylase.
National Institute of Diabetes and Digestive and Kidney Diseases
P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.
National Institute of Diabetes and Digestive and Kidney Diseases
Bidirectional, iterative approach to the structural delineation of the functional"chemoprint" in GPR40 for agonist recognition.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.
National Institute of Diabetes and Digestive and Kidney Diseases
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
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
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
(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
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of pyrimidine nucleotides containing a 5'-α,β-methylene diphosphonate at the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.
National Institute of Diabetes and Digestive and Kidney Diseases
Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase.
National Institute of Diabetes and Digestive and Kidney Diseases
Biological Evaluation of 5'-(
National Institute of Diabetes and Digestive and Kidney Diseases
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.
National Institute of Diabetes and Digestive and Kidney Diseases
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Syntheses of (R)- and (S)-2- and 6-fluoronorepinephrine and (R)- and (S)-2- and 6-fluoroepinephrine: effect of stereochemistry on fluorine-induced adrenergic selectivities.
National Institute of Diabetes and Digestive and Kidney Diseases
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity.
National Institute of Diabetes and Digestive and Kidney Diseases
(Aminoalkyl)indole isothiocyanates as potential electrophilic affinity ligands for the brain cannabinoid receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Design, Synthesis by Click Chemistry and
National Institute of Diabetes and Digestive and Kidney Diseases
4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel site-directed affinity ligands for GABA-gated chloride channels: synthesis, characterization, and molecular modeling of 1-(isothiocyanatophenyl)-4-tert-butyl-2,6,7-trioxabicyclo[2.2.2]octanes .
National Institute of Diabetes and Digestive and Kidney Diseases
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.
The Scripps Research Institute
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Genentech