Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides

…, HF Campbell, S Klein, JE Airey, P Darkes…

Index: Youssefyeh; Campbell; Klein; Airey; Darkes; Powers; Schnapper; Neuenschwander; Fitzpatrick; Pendley; Martin Journal of Medicinal Chemistry, 1992 , vol. 35, # 5 p. 895 - 903

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Citation Number: 22

Abstract

This report describes the development of novel benzamides which are orally active, highly potent, specific antagonists of 5-HT3 receptors. Described in this fist report are the structure- activity relationships that led to novel structures with improved potency and selectivity. From this series of compounds,(S)-28 was identified and selected for further evaluation as a 5- HT3 receptor antagonist. Compared with 5-HT3 antagonists such as GR 38032F, BRL ...