The discovery and SAR of indoline-3-carboxamides—a new series of 5-HT 6 antagonists

…, R Gilfillan, R Goodwin, D Jaap, EC O'Donnell…

Index: Reid, Mark; Carlyle, Ian; Caulfield, Wilson L.; Clarkson, Tom R.; Cusick, Fiona; Epemolu, Ola; Gilfillan, Robert; Goodwin, Richard; Jaap, David; O'Donnell, Elise C.; Presland, Jeremy; Rankovic, Zoran; Spinks, Daniel; Spinks, Gayle; Thomson, Anne M.; Thomson, Fiona; Strain, James; Wishart, Grant Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3713 - 3716

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Citation Number: 7

Abstract

Antagonists of the 5-HT6 receptor have been shown to improve cognitive function in a wide range of animal models and as such may prove to be attractive agents for the symptomatic treatment of cognitive disorders such as Alzheimer's disease (AD) and schizophrenia. We report herein the identification and SAR around N-(2-aminoalkyl)-1-(arylsulfonyl) indoline-3- carboxamides—a novel chemotype of 5-HT6 antagonists.