373 articles for thisTarget
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Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT
Suven Life Sciences
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Virginia Commonwealth University
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
The University of Newcastle
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.
Meiji Seika Kaisha
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Glaxosmithkline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Glaxosmithkline
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Glaxosmithkline
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
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics.
Huazhong University of Science and Technology
Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT
Jagiellonian University Collegium Medicum
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.
Eli Lilly
Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5-HT
University of Montreal
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.
University of Bari Aldo Moro
1-Sulfonyl-6-Piperazinyl-7-Azaindoles as potent and pseudo-selective 5-HT6 receptor antagonists.
Selvita
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.
Abbott Healthcare Products
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
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University of Illinois At Chicago
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.
National Institute of Biological Sciences, Beijing
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
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.
City University of New York
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
City University of New York
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
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
University of Illinois At Chicago
6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands.
Universities of Lille
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
Jagiellonian University Collegium Medicum
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
Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands.
Jagiellonian University
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.
Ewha Womans University
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
Yonsei University
Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.
Universidad Complutense De Madrid
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
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands.
University of Copenhagen
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors.
Pfizer
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.
Adamed
Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists.
Cephalon
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects.
Therachem Research Medilab (India)
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
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.
Glaxosmithkline
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.
Universidad Complutense
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
H. Lundbeck
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
Synthesis and in vivo evaluation of [O-methyl-11C] N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzenesulfonamide as an imaging probe for 5-HT6 receptors.
Columbia University Medical Center
Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
QSAR studies of bioactivities of 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 receptor ligands using physicochemical descriptors and MLR and ANN-modeling.
Islamic Azad University
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Schering-Plough Research Institute
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism.
Roche Palo Alto
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Glaxosmithkline
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Glaxosmithkline
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Glaxosmithkline
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
F. Hoffmann-La Roche
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Organon Research and Development Group
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Smithkline Beecham Pharmaceuticals
Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands.
Suven Life Sciences
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
Neurosearch Sweden
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University of Sydney
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
University of Caen Normandie
Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines-Synthesis and 'structure-activity' relationship.
Chemical Diversity Research Institute
N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists.
Suven Life Sciences
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
National Institute of Biological Sciences
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists.
TBA
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.
University of North Carolina At Chapel Hill
Microwave assisted synthesis of spirocyclic pyrrolidines -s1 receptor ligands with modified benzene-N-distance.
Institut F£R Pharmazeutische Und Medizinische Chemie
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.
Pfizer
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists.
Ewha Womans University
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
University of Namur
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
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
Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.
Chemical Diversity Research Institute
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.
Universidad Complutense De Madrid
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
Universitat De Barcelona
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Purdue University
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.
Egis Pharmaceuticals
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.
F. Hoffmann-La Roche
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
F. Hoffmann-La Roche
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Wyeth Research
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.
Virginia Commonwealth University
Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Virginia Commonwealth University
Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors.
Virginia Commonwealth University
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
Alcon Research
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
Virginia Commonwealth University
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).
Purdue University
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
Eli Lilly
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.
Astra Arcus
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
Virginia Commonwealth University
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
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
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.
Cephalon
Synthesis and structure-activity relationship (SAR) of (5,7-disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as potent serotonin 5-HT(6) receptor (5-HT(6)R) antagonists.
Chemical Diversity Research Institute
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.
Jagiellonian University Medical College
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features.
Abbott Healthcare Products
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.
Green Cross
Rigidized 1-aryl sulfonyl tryptamines: synthesis and pharmacological evaluation as 5-HT6 receptor ligands.
Suven Life Sciences
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
University of Copenhagen
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.
Wyeth Research
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.
TBA
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Pfizer
2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: new series of highly potent and specific serotonin 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.
Wyeth Research
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.
The University of Sydney
Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists.
Suven Life Sciences
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.
Korea Research Institute of Chemical Technology
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.
Wyeth Research
Development of molecular probes for the human 5-HT(6) receptor.
Universidad Complutense De Madrid
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.
Korea Research Institute of Chemical Technology
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Yangji Chemicals
Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Green Cross
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.
Wyeth Pharmaceuticals
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.
Wyeth Research
Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
Chemical Diversity Research Institute
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.
Wyeth Research
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Wyeth Research
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.
Universitat De Barcelona
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.
Novartis Institutes For Biomedical Research
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Roche Palo Alto
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.
Korea Research Institute of Chemical Technology
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
Florida A&M University
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands.
Wyeth Research
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Glaxosmithkline
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
Wyeth Research
Preparation of piperazine derivatives as 5-HT7 receptor antagonists.
Ewha Womans University
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Uppsala University
Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.
Virginia Commonwealth University
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Korea Research Institute of Chemical Technology
Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.
Wyeth Research
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
Hybrid molecules combining GABA-A and serotonin 5-HT
Jagiellonian University Medical College
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
Jagiellonian University Medical College
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.
Virginia Commonwealth University
Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT
University of Sassari
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.
Virginia Commonwealth University
Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
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
New N-aryl-N'-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT
Cracow University of Technology
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
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Alcon Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
F. Hoffmann-La Roche
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors.
Virginia Commonwealth University
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists.
Wyeth Research
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Carlsson Research
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT
Hec Pharm Group
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
Virginia Commonwealth University
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
Laboratorios Dr. Esteve
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
Beijing Normal University
Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HT
Hec Research and Development Center
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Wyeth Research
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Wyeth Research
Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.
Jagiellonian University Medical College
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Merck
Discovery of G Protein-Biased Ligands against 5-HT
Korea Institute of Science and Technology
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
Uppsala University
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 and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT
Jagiellonian University Medical College
Discovery of G Protein-Biased Antagonists against 5-HT
Korea Institute of Science and Technology
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Cracow University of Technology
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
Huazhong University of Science and Technology
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
Bristol-Myers Squibb Pharmaceutical Research Institute
N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates.
Virginia Commonwealth University
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.
Eli Lilly
Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
University of Perugia
Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT
Polish Academy of Sciences
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
Normandie Univ
Identification of a novel series of selective 5-HT7 receptor antagonists.
Glaxosmithkline
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
Jiangsu Ocean University
Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT4R) partial agonist and 5-HT6R antagonist activities, as potential treatment of Alzheimer's disease.
Normandie Universit£
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
Westf£Lische Wilhelms-Universit£T M£Nster
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands.
Nps Pharmaceuticals
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.
Yale University
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
Jagiellonian University Medical College
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
Merck Sharp & Dohme Research Laboratories
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Polish Academy of Sciences
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.
Cracow University of Technology
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
Glaxosmithkline
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT
City University of New York
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College of Physicians and Surgeons
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Virginia Commonwealth University
Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands.
Gedeon Richter
6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.
Nps Allelix
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.
Jagiellonian University Medical College
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Virginia Commonwealth University
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
Merck Sharp & Dohme Research Laboratories
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
Medical University of Warsaw
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
Knoll Pharmaceuticals
Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT
Polish Academy of Sciences
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.
Cracow University of Technology
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.
Agouron Pharmaceuticals
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
Medical University of Warsaw
Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT
Jagiellonian University
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
Northwest University
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Medical University of Warsaw
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.
Cracow University of Technology
Synthesis of azepino[4,5-b]indol-4-ones via MCR/free radical cyclization and in vitro-in silico studies as 5-Ht₆R ligands.
Universidad De Guanajuato
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a]pyrimidin-4-imines as potent 5-HT₆ antagonists.
Bristol-Myers Squibb Research and Development
Design and synthesis of novel series of 5-HT6 receptor ligands having indole, a central aromatic core and 1-amino-4 methyl piperazine as a positive ionizable group.
Ewha Womans University
Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.
Chemical Diversity Research Institute (Cdri)
Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment.
Korea Institute of Science & Technology (Kist)
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Jagiellonian University Medical College
Benzenesulfonyl and Benzenesulfonamide as Modulators of the 5-HT6 Receptor: Patent Highlight.
Dart Neuroscience
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
Roche Pharmaceuticals
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
Glaxosmithkline
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Solvay Pharma
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Glaxosmithkline
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Glaxosmithkline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Glaxosmithkline
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
Glaxosmithkline R&D
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
Meiji Seika Kaisha
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Huazhong University of Science and Technology
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Jagiellonian University Medical College
Discovery of β-Arrestin Biased Ligands of 5-HT
Korea Institute of Science and Technology
Structure-Activity Relationships and Therapeutic Potentials of 5-HT
University of Catania
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
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.
University of The Philippines
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structural insights into serotonin receptor ligands polypharmacology.
Polish Academy of Sciences
Novel naphthyloxy derivatives - Potent histamine H
Jagiellonian University Medical College
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT
University of Science and Technology
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
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
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
EPOXYAMIDES AS KRAS G12C AND KRAS G12D INHIBITORS AND METHODS OF USING THE SAME
Amgen
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
2-phenyl-3,4-dihydropyrrolo[2,1-Ff] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof
Topadur Pharma
Pyrrole heteroaryl ring derivative and method of use thereof
Jiangsu Hengrui Medicine
C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
TBA
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Inhibitors of PTP4A3 for the treatment of cancer
University of Virginia Patent Foundation
Specific inhibitors of cytochrome P450 26 retinoic acid hydroxylase
University of Washington Through Its Center For Commercialization
Quinazoline derivatives substituted by aniline, preparation method and use thereof
Xuanzhu Pharma
Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
Taiho Pharmaceutical
Design, Synthesis and Biological Evaluation of Peptidyl Epoxyketone Proteasome Inhibitors Composed of ??????-amino Acids.
Zhejiang University
Pseudodipeptides as MMP inhibitors
French Alternative Energies and Atomic Energy Commission
Triazolo and tetrazolo pyrimidine derivatives as HNE inhibitors for treating COPD
Bayer Intellectual Property
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.
Roche Bioscience
URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.
University of California Irvine
Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation.
Tohoku University
Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.
Massachusetts Institute of Technology
Chemical library screens targeting an HIV-1 accessory factor/host cell kinase complex identify novel antiretroviral compounds.
University of Pittsburgh
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
Thermodynamics of the molecular and chiral recognition of cycloalkanols and camphor by modified beta-cyclodextrins possessing simple aromatic tethers.
Nankai University
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.
Dainippon Sumitomo Pharma
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Wyeth Research
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.
Cnr
Identification of inhibitors of checkpoint kinase 1 through template screening.
The Institute of Cancer Research
Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.
Purdue University
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Yale University
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood.
Wyeth Research
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
Universita Di Siena
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Kudos Pharmaceuticals
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Tanabe Research Laboratories Usa
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb