Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands

…, R Kambhampati, AV Daulatabad, P Gudla…

Index: Nirogia, Ramakrishna V.S.; Kambhampati, Ramasastri; Daulatabad, Anand V.; Gudla, Parandhama; Shaikh, Mohammad; Achanta, Pramod Kumar; Shinde, Anil K.; Dubey, Pramod Kumar Journal of Enzyme Inhibition and Medicinal Chemistry, 2011 , vol. 26, # 3 p. 341 - 349

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Citation Number: 7

Abstract

A series of novel conformationally restricted N1-arylsulfonyl-3-aminoalkoxy indoles were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. Many of the synthesized compounds have moderate in vitro-binding affinities at 5-HT6R. The lead compound 8b (% inhibition= 97.2 at 1 μM) from this series has good pharmacokinetic profile in male Wister rats and is active in animal model of cognition like Morris water maze. The details of ...