The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28212021 |
111 |
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 |
28244748 |
119 |
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
Virginia Commonwealth University |
27997171 |
48 |
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. |
The University of Newcastle |
28435524 |
47 |
Pyrano[2,3,4- |
Polish Academy of Sciences |
12467617 |
17 |
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. |
Meiji Seika Kaisha |
12392747 |
36 |
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Glaxosmithkline |
11992776 |
70 |
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists. |
Glaxosmithkline |
11266169 |
27 |
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor. |
Smithkline Beecham Pharmaceuticals |
11597412 |
116 |
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor. |
Glaxosmithkline |
27876250 |
60 |
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 |
27639363 |
141 |
Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. |
Huazhong University of Science and Technology |
27560283 |
58 |
Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
Jagiellonian University Collegium Medicum |
27908761 |
55 |
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. |
Eli Lilly |
28029458 |
50 |
Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5-HT |
Universit£ |
27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
27318552 |
126 |
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. |
Universit£ |
27117428 |
50 |
1-Sulfonyl-6-Piperazinyl-7-Azaindoles as potent and pseudo-selective 5-HT6 receptor antagonists. |
Selvita |
26876931 |
36 |
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket. |
Abbott Healthcare Products |
26819658 |
30 |
Sulfonamide Derivatives and Pharmaceutical Applications Thereof. |
Temple University |
26988801 |
55 |
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 |
26704965 |
229 |
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 |
26700945 |
68 |
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 |
26852005 |
82 |
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists. |
Yonsei University |
26698537 |
93 |
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 |
26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
26475518 |
19 |
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor. |
City University of New York |
26099069 |
15 |
Therapeutic Potential of 5-HT6 Receptor Agonists. |
Universit£ |
26227772 |
22 |
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity. |
City University of New York |
25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University of New York |
25965777 |
58 |
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 |
25633969 |
96 |
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
University of Illinois At Chicago |
25637882 |
2 |
6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands. |
Universities of Lille |
25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
25555143 |
60 |
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 |
25866241 |
88 |
Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands. |
Jagiellonian University |
25684421 |
24 |
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists. |
Ewha Womans University |
25127461 |
36 |
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression. |
Yonsei University |
24850589 |
71 |
Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease. |
Universidad Complutense De Madrid |
25435254 |
82 |
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 |
24878269 |
50 |
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. |
University of Copenhagen |
24878222 |
50 |
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 |
24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
24704027 |
31 |
Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists. |
Cephalon |
24900826 |
22 |
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects. |
Therachem Research Medilab (India) |
24900821 |
5 |
Quinoline Derivatives as 5-HT6 Receptor PET Ligands. |
Dart Neuroscience |
24691057 |
62 |
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 |
16730983 |
165 |
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation. |
Glaxosmithkline |
15974573 |
46 |
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists. |
Universidad Complutense |
23218776 |
45 |
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
H. Lundbeck |
23279866 |
69 |
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 |
21821420 |
1 |
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 |
21277782 |
36 |
Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
20547432 |
52 |
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 |
20471831 |
31 |
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists. |
Schering-Plough Research Institute |
20434910 |
60 |
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism. |
Roche Palo Alto |
19146417 |
70 |
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor. |
Glaxosmithkline |
18829312 |
64 |
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity. |
Glaxosmithkline |
18433113 |
124 |
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
Glaxosmithkline |
12646038 |
19 |
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 |
11140733 |
92 |
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 |
23141912 |
30 |
Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands. |
Suven Life Sciences |
23043306 |
69 |
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 |
22959245 |
175 |
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 |
21486038 |
177 |
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. |
H. Lundbeck |
23641311 |
38 |
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design. |
TBA |
23102207 |
122 |
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. |
Universit£ |
22664127 |
19 |
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 |
23036955 |
59 |
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 |
22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
National Institute of Biological Sciences |
22926225 |
200 |
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 |
22537153 |
10 |
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 |
22578786 |
40 |
Microwave assisted synthesis of spirocyclic pyrrolidines -s1 receptor ligands with modified benzene-N-distance. |
Institut F£R Pharmazeutische Und Medizinische Chemie |
22313242 |
146 |
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. |
Pfizer |
22313227 |
78 |
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 |
22405919 |
3 |
Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists. |
Ewha Womans University |
21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
University of Namur |
21207959 |
69 |
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 |
20931963 |
112 |
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 |
20541425 |
191 |
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 |
20560595 |
21 |
(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 |
19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
Hunter College and The Graduate Center of The City University of New York |
20078106 |
50 |
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation. |
Universidad Complutense De Madrid |
19159187 |
38 |
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists. |
Universitat De Barcelona |
18468904 |
48 |
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 |
18361484 |
61 |
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists. |
Egis Pharmaceuticals |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
18023344 |
77 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. |
F. Hoffmann-La Roche |
17998160 |
101 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. |
F. Hoffmann-La Roche |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
15658848 |
103 |
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. |
Wyeth Research |
15745826 |
22 |
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. |
Virginia Commonwealth University |
15990303 |
16 |
Interaction of chiral MS-245 analogs at h5-HT6 receptors. |
Virginia Commonwealth University |
15357994 |
13 |
Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors. |
Virginia Commonwealth University |
12954071 |
109 |
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 |
12825922 |
207 |
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
Virginia Commonwealth University |
12213075 |
70 |
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 |
11708905 |
20 |
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 |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
15050637 |
19 |
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands. |
Virginia Commonwealth University |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
22290076 |
44 |
Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists. |
Amri |
22277589 |
72 |
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 |
22226656 |
75 |
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 |
22153937 |
52 |
Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists. |
Cephalon |
22029285 |
6 |
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 |
22001327 |
77 |
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands. |
Jagiellonian University Medical College |
21866910 |
66 |
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features. |
Abbott Healthcare Products |
21823597 |
373 |
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter. |
Green Cross |
21724392 |
3 |
Rigidized 1-aryl sulfonyl tryptamines: synthesis and pharmacological evaluation as 5-HT6 receptor ligands. |
Suven Life Sciences |
20719507 |
37 |
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 |
19443217 |
60 |
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
19433358 |
19 |
Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands. |
Wyeth Research |
24900216 |
33 |
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands. |
TBA |
21195614 |
56 |
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 |
21333408 |
21 |
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 |
21093272 |
126 |
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. |
Wyeth Research |
21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
The University of Sydney |
21134749 |
31 |
Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists. |
Suven Life Sciences |
21190848 |
61 |
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands. |
Korea Research Institute of Chemical Technology |
20949929 |
63 |
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb |
20932009 |
127 |
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. |
Wyeth Research |
20845907 |
14 |
Development of molecular probes for the human 5-HT(6) receptor. |
Universidad Complutense De Madrid |
20812727 |
157 |
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 |
20655748 |
92 |
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents. |
Korea Research Institute of Chemical Technology |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
19939513 |
21 |
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
20223662 |
174 |
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists. |
Yangji Chemicals |
20207539 |
15 |
Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
20149649 |
133 |
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. |
Green Cross |
20138763 |
50 |
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators. |
Wyeth Pharmaceuticals |
20170099 |
58 |
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. |
Wyeth Research |
19945877 |
50 |
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 |
19646882 |
72 |
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 |
19884004 |
20 |
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands. |
Wyeth Research |
19523834 |
79 |
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. |
Wyeth Research |
19739674 |
39 |
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists. |
Universitat De Barcelona |
19783143 |
65 |
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 |
19329329 |
183 |
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 |
19231180 |
81 |
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 |
19152787 |
29 |
Identification of a series of benzoxazoles as potent 5-HT6 ligands. |
Wyeth Research |
18602261 |
65 |
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 |
18595716 |
142 |
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 |
18583130 |
25 |
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands. |
Wyeth Research |
18573659 |
47 |
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. |
Glaxosmithkline |
18557608 |
108 |
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors. |
Wyeth Research |
18456500 |
56 |
Preparation of piperazine derivatives as 5-HT7 receptor antagonists. |
Ewha Womans University |
17067154 |
27 |
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. |
Uppsala University |
18201064 |
12 |
Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies. |
Virginia Commonwealth University |
18053713 |
78 |
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 |
17892934 |
37 |
Discovery of 5-HT6 receptor ligands based on virtual HTS. |
4Sc |
17624788 |
104 |
Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists. |
Wyeth Research |
17571866 |
49 |
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 |
17524641 |
69 |
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists. |
Glaxosmithkline |
17239595 |
23 |
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors. |
Virginia Commonwealth University |
16945532 |
8 |
Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors. |
Virginia Commonwealth University |
16913710 |
18 |
Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors. |
Virginia Commonwealth University |
16722631 |
87 |
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 |
16709453 |
6 |
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. |
Virginia Commonwealth University |
16458504 |
37 |
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 |
16392816 |
113 |
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. |
Alcon Research |
16392798 |
46 |
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 |
16361098 |
70 |
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 |
16183286 |
9 |
Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors. |
Virginia Commonwealth University |
16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College of Physicians and Surgeons |
16125933 |
114 |
Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists. |
Wyeth Research |
16055331 |
45 |
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
Carlsson Research |
15808453 |
14 |
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. |
Virginia Commonwealth University |
15771424 |
74 |
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. |
Laboratorios Dr. Esteve |
15603958 |
77 |
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists. |
Wyeth Research |
15482912 |
24 |
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands. |
Wyeth Research |
15261279 |
27 |
Aminotriazine 5-HT7 antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
14761190 |
10 |
Recognition of privileged structures by G-protein coupled receptors. |
Novo Nordisk |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
14584934 |
15 |
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 |
12951125 |
18 |
N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates. |
Virginia Commonwealth University |
12825944 |
184 |
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 |
12643910 |
55 |
Identification of a novel series of selective 5-HT7 receptor antagonists. |
Glaxosmithkline |
12361399 |
17 |
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
Universita Di Camerino |
12161155 |
33 |
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands. |
Nps Pharmaceuticals |
12014970 |
42 |
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging. |
Yale University |
11689074 |
112 |
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. |
Merck Sharp & Dohme Research Laboratories |
32247749 |
119 |
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs. |
Cracow University of Technology |
11514164 |
36 |
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists. |
Glaxosmithkline |
32631561 |
110 |
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
City University of New York |
11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College of Physicians and Surgeons |
32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
11055342 |
21 |
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. |
Virginia Commonwealth University |
27496213 |
98 |
Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands. |
Gedeon Richter |
10937732 |
15 |
6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists. |
Nps Allelix |
27326337 |
126 |
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
Jagiellonian University Medical College |
10715164 |
57 |
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
Virginia Commonwealth University |
32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
30703658 |
79 |
Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
Medical University of Warsaw |
30904783 |
146 |
Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT |
Polish Academy of Sciences |
30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
University of North Carolina At Chapel Hill |
31253535 |
115 |
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants. |
Cracow University of Technology |
31253532 |
85 |
New dual ligands for the D |
Cracow University of Technology |
10201844 |
24 |
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 |
31325785 |
92 |
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 |
31229876 |
89 |
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 |
31229883 |
202 |
2-Aminoimidazole-based antagonists of the 5-HT |
Polish Academy of Sciences |
31009908 |
28 |
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
Northwest University |
31401465 |
52 |
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
Julius Maximilian University of W£Rzburg |
31734022 |
133 |
Virtual screening-driven discovery of dual 5-HT |
Polish Academy of Sciences |
31586817 |
96 |
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 |
31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
31547945 |
88 |
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives. |
Cracow University of Technology |
26996373 |
5 |
Synthesis of azepino[4,5-b]indol-4-ones via MCR/free radical cyclization and in vitro-in silico studies as 5-Ht?R ligands. |
Universidad De Guanajuato |
26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
25052427 |
2 |
The use of spirocyclic scaffolds in drug discovery. |
Vitae Pharmaceuticals |
24495863 |
35 |
Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a]pyrimidin-4-imines as potent 5-HT? antagonists. |
Bristol-Myers Squibb Research and Development |
23810425 |
10 |
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 |
23787290 |
20 |
Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-??6 receptors. |
Chemical Diversity Research Institute (Cdri) |
23820387 |
9 |
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) |
23787101 |
33 |
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
Jagiellonian University Medical College |
30496988 |
25 |
Pharmaceutical and medicinal significance of sulfur (S |
Wuhan University of Technology |
24900400 |
18 |
Benzenesulfonyl and Benzenesulfonamide as Modulators of the 5-HT6 Receptor: Patent Highlight. |
Dart Neuroscience |
21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
17485206 |
28 |
3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists. |
Roche Pharmaceuticals |
17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
16143522 |
27 |
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists. |
Glaxosmithkline |
15887956 |
77 |
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. |
Glaxosmithkline |
16002289 |
65 |
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. |
Glaxosmithkline |
14613313 |
34 |
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp. |
Glaxosmithkline R&D |
12014957 |
86 |
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor. |
Meiji Seika Kaisha |
10052959 |
20 |
Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor. |
Meiji Seika Kaisha |
30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
30389290 |
146 |
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. |
Texas Tech University Health Sciences Center |
29407591 |
276 |
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects. |
Jagiellonian University Medical College |
30028132 |
135 |
Discovery of ?-Arrestin Biased Ligands of 5-HT |
Korea Institute of Science and Technology |
29767995 |
34 |
Structure-Activity Relationships and Therapeutic Potentials of 5-HT |
Universit£ |
29910079 |
50 |
Spiro[pyrrolidine-3,3'-oxindoles] as 5-HT |
Hungarian Academy of Sciences |
29730027 |
99 |
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 |
28745513 |
309 |
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products. |
University of The Philippines |
29767967 |
74 |
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y |
National Institute of Diabetes and Digestive and Kidney Diseases |
28391970 |
30 |
Novel 5-HT |
Jagiellonian University Medical College |
29679900 |
36 |
Structural insights into serotonin receptor ligands polypharmacology. |
Polish Academy of Sciences |
29291439 |
74 |
Novel non-sulfonamide 5-HT |
Palack£ |
29853337 |
11 |
Pyrroloquinoline scaffold-based 5-HT |
Jagiellonian University Medical College |
29681486 |
33 |
Novel naphthyloxy derivatives - Potent histamine H |
Jagiellonian University Medical College |
29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
28729057 |
11 |
Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT |
University of Science and Technology |
28776992 |
110 |
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. |
Northwestern University |
28763213 |
193 |
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 |
28489950 |
119 |
Return of D |
University of Nebraska Medical Center |
28529043 |
75 |
The impact of the halogen bonding on D |
Jagiellonian University Medical College |
28441580 |
23 |
The computer-aided discovery of novel family of the 5-HT |
Jagiellonian University |
24753254 |
2 |
Functional rescue of Kallmann syndrome-associated prokineticin receptor 2 (PKR2) mutants deficient in trafficking. |
Central South University |
28267984 |
35 |
Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's disease. |
Sichuan University |
28043716 |
18 |
Synthesis, molecular docking studies of hybrid benzimidazole as a-glucosidase inhibitor. |
Universiti Teknologi Mara (Uitm) |
28043719 |
30 |
Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives. |
Cumhuriyet University |
23615903 |
8 |
The A128T resistance mutation reveals aberrant protein multimerization as the primary mechanism of action of allosteric HIV-1 integrase inhibitors. |
The Ohio State University |
23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University of Washington |
26077890 |
33 |
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids. |
Tehran University of Medical Sciences |
26218629 |
26 |
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1). |
Oregon Health & Science University |
25965977 |
15 |
Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers. |
Panjab University |
11579444 |
23 |
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA. |
The Royal Danish School of Pharmacy |
11259544 |
7 |
Zebra finch CB1 cannabinoid receptor: pharmacology and in vivo and in vitro effects of activation. |
Florida State University |
9536007 |
23 |
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach. |
University of Bonn |
8867105 |
49 |
Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons. |
Cnrs Upr 9023 |
8391122 |
35 |
Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. |
Merck Sharp & Dohme Research Laboratories |
8386236 |
11 |
In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist. |
Whitby Research |
16647257 |
17 |
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity. |
Johnson & Johnson Pharmaceutical |