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

doi:10.1007/s12039-015-0800-7

Paper

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

Published Apr 16, 2015 · R. Nirogi, R. Badange, Kiran Kumar Kandukuri

Journal of Chemical Sciences

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Abstract

In continuation to our efforts to develop better treatment options for cognitive decline, we have been focussing on 5-HT_6 receptor (5-HT_6R) 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-HT_6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT_6R, good pharmacokinetic profile, excellent selectivity and no Cytochrome P450 liabilities. We report a novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives as potent and selective 5-HT_6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT_6R, good pharmacokinetic profile, excellent selectivity and no CYP liabilities.

Study Snapshot

The novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives] show potent and selective 5-HT6 receptor antagonists with good pharmacokinetic profile and no Cytochrome

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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

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