[3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indoles: Synthesis, SAR and biological evaluation as a novel class of 5-HT6 Receptor Antagonists

Autor:	Mukkanti Khagga, Rajesh Kumar Badange, Ramakrishna Nirogi, Kiran Kumar Kandukuri
Rok vydání:	2015
Předmět:	biology Stereochemistry Cytochrome P450 General Chemistry chemistry.chemical_compound chemistry biology.protein 5-HT6 receptor Structure–activity relationship Cognitive decline Receptor Selectivity Lead compound Biological evaluation
Zdroj:	Journal of Chemical Sciences. 127:439-445
ISSN:	0973-7103 0974-3626
DOI:	10.1007/s12039-015-0800-7
Popis:	In continuation to our efforts to develop better treatment options for cognitive decline, we have been focussing on 5-HT6 receptor (5-HT6R) antagonists, which are known to be involved in improving cognitive function in numerous animal models. In this paper, we report a novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives as potent and selective 5-HT6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT6R, good pharmacokinetic profile, excellent selectivity and no Cytochrome P450 liabilities.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::4835744ffbb3ae34f5c5ea0affa26b3a https://doi.org/10.1007/s12039-015-0800-7 Zobrazit plný text záznamu Plný text ve formátu PDF