108 articles for thisTarget
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Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation.
Jagiellonian University Medical College
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
Design, synthesis, and biological evaluation of fluorinated imidazo[1,2-a]pyridine derivatives with potential antipsychotic activity.
Jagiellonian University Medical College
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.
Jagiellonian University Medical College
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines asa
Jagiellonian University Medical College
Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems.
Jagiellonian University Medical College
Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.
Jagiellonian University Medical College
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
Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.
Jagiellonian University Medical College
Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.
Jagiellonian University Medical College
N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile.
Jagiellonian University Medical College
Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents.
Jagiellonian University Medical College
(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.
Jagiellonian University Medical College
Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Jagiellonian University Medical College
Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.
Jagiellonian University Medical College
Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides.
Jagiellonian University Medical College
Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
Jagiellonian University Medical College
Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase andß-amyloid aggregation inhibitors with neuroprotective properties.
Jagiellonian University Medical College
Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.
Jagiellonian University Medical College
Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives.
Jagiellonian University Medical College
a-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
Jagiellonian University Medical College
Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents.
Jagiellonian University Medical College
Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT1A receptor functional profile.
Jagiellonian University Medical College
Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.
Jagiellonian University Medical College
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.
Jagiellonian University Medical College
SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.
Jagiellonian University Medical College
Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands.
Jagiellonian University Medical College
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors.
Jagiellonian University Medical College
Novel alkyl- and arylcarbamate derivatives with N-benzylpiperidine and N-benzylpiperazine moieties as cholinesterases inhibitors.
Jagiellonian University Medical College
Search for influence of spatial properties on affinity ata1-adrenoceptor subtypes for phenylpiperazine derivatives of phenytoin.
Jagiellonian University Medical College
Design, synthesis and pharmacological evaluation of new 1-[3-(4-arylpiperazin-1-yl)-2-hydroxy-propyl]-3,3-diphenylpyrrolidin-2-one derivatives with antiarrhythmic, antihypertensive, and alpha-adrenolytic activity.
Jagiellonian University Medical College
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.
Jagiellonian University Medical College
Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.
Jagiellonian University Medical College
The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.
Jagiellonian University Medical College
Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
Jagiellonian University Medical College
7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands.
Jagiellonian University Medical College
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.
Jagiellonian University Medical College
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.
Jagiellonian University Medical College
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
Jagiellonian University Medical College
Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity.
Jagiellonian University Medical College
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Jagiellonian University Medical College
Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives.
Jagiellonian University Medical College
Preliminary evaluation of pharmacological properties of some xanthone derivatives.
Jagiellonian University Medical College
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Jagiellonian University Medical College
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
Novel drug-like fluorenyl derivatives as selective butyrylcholinesterase and β-amyloid inhibitors for the treatment of Alzheimer's disease.
Jagiellonian University Medical College
Hybrid molecules combining GABA-A and serotonin 5-HT
Jagiellonian University Medical College
Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies.
Jagiellonian University Medical College
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
Jagiellonian University Medical College
Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Jagiellonian University Medical College
Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Jagiellonian University Medical College
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
Jagiellonian University Medical College
Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.
Jagiellonian University Medical College
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT
Jagiellonian University Medical College
Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity.
Jagiellonian University Medical College
Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT
Jagiellonian University Medical College
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters.
Jagiellonian University Medical College
Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT
Jagiellonian University Medical College
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
Jagiellonian University Medical College
Structural modifications in the distal, regulatory region of histamine H
Jagiellonian University Medical College
Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.
Jagiellonian University Medical College
Novel Aryloxyethyl Derivatives of 1-(1-Benzoylpiperidin-4-yl)methanamine as the Extracellular Regulated Kinases 1/2 (ERK1/2) Phosphorylation-Preferring Serotonin 5-HT
Jagiellonian University Medical College
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H
Jagiellonian University Medical College
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
Jagiellonian University Medical College
Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT
Jagiellonian University Medical College
In silico and in vitro studies on interaction of novel non-imidazole histamine H
Jagiellonian University Medical College
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
Alkyl derivatives of 1,3,5-triazine as histamine H
Jagiellonian University Medical College
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H
Jagiellonian University Medical College
Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands.
Jagiellonian University Medical College
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.
Jagiellonian University Medical College
Optimization and preclinical evaluation of novel histamine H
Jagiellonian University Medical College
1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
Jagiellonian University Medical College
Search for new multi-target compounds against Alzheimer's disease among histamine H
Jagiellonian University Medical College
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.
Jagiellonian University Medical College
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
Jagiellonian University Medical College
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
Jagiellonian University Medical College
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
Jagiellonian University Medical College
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Jagiellonian University Medical College
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.
Jagiellonian University Medical College
Serotonin transporter activity of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives in aspect of their acid-base properties.
Jagiellonian University Medical College
Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α₁-adrenoceptor antagonistic properties.
Jagiellonian University Medical College
Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with α₁-adrenoceptor affinities.
Jagiellonian University Medical College
Pharmacophore models based studies on the affinity and selectivity toward 5-HT1A with reference to α1-adrenergic receptors among arylpiperazine derivatives of phenytoin.
Jagiellonian University Medical College
Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.
Jagiellonian University Medical College
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Jagiellonian University Medical College
Synthesis and biological activity of novel tert-amylphenoxyalkyl (homo)piperidine derivatives as histamine H
Jagiellonian University Medical College
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.
Jagiellonian University Medical College
Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors.
Jagiellonian University Medical College
MF-8, a novel promising arylpiperazine-hydantoin based 5-HT
Jagiellonian University Medical College
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
Jagiellonian University Medical College
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT
Jagiellonian University Medical College
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
Jagiellonian University Medical College
Novel naphthyloxy derivatives - Potent histamine H
Jagiellonian University Medical College
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
Jagiellonian University Medical College
Triazolo and tetrazolo pyrimidine derivatives as HNE inhibitors for treating COPD
Bayer Intellectual Property
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
Acadia Pharmaceuticals