Structure–activity relationship of 5-chloro-2-methyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H-indole analogues as 5-HT 6 receptor agonists

…, P Svensson, H Boettcher, C Sonesson

Index: Mattsson, Cecilia; Svensson, Peder; Boettcher, Henning; Sonesson, Clas European Journal of Medicinal Chemistry, 2013 , vol. 63, p. 578 - 588

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Citation Number: 2

Abstract

To further investigate the structure–activity relationship (SAR) of the 5-hydroxytryptamine type 6 (5-HT6) receptor agonist 5-chloro-2-methyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H- indole (EMD386088, 6), a series of 2-methyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H-indoles were synthesized, and in vitro affinity to, and functional activity at 5-HT6 receptors was tested. We focused on substituents made at the indole N1-, 2-and 5-positions and these ...