Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands

Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimer's disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor-one of the emerging therapeuti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-06, Vol.19 (12), p.3214-3216
Main Authors: LIU, Kevin G, LO, Jennifer R, ROBICHAUD, Albert J, COMERY, Thomas A, GUO MING ZHANG, ZHANG, Jean Y, KOWAL, Dianne M, SMITH, Deborah L, LI DI, KERNS, Edward H, SCHECHTER, Lee E
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cognition Disorders - drug therapy
Dementia - drug therapy
Humans
Indazoles - chemical synthesis
Indazoles - pharmacology
Ligands
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperidines - chemical synthesis
Piperidines - pharmacology
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Receptors, Serotonin - drug effects
Serotonin Antagonists - chemical synthesis
Serotonin Antagonists - pharmacology
Serotoninergic system
Sulfinic Acids - chemical synthesis
Sulfinic Acids - pharmacology
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Summary:Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimer's disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor-one of the emerging therapeutic targets in this area. Herein, we report the identification of a novel series of 3-piperidinyl-5-sulfonylindazole derivatives as potent 5-HT(6) antagonists. The synthesis and SAR of this class of compounds are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.04.108