Substituted benzamides. 1. Potential nondopaminergic antagonists of chemotherapy-induced nausea and emesis

I Monkovic, D Willner, MA Adam, M Brown…

Index: Monkovic, Ivo; Wllner, David; Adam, Michael A.; Brown, Myron; Crenshaw, R. R.; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1548 - 1557

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Citation Number: 26

Abstract

A series of new substituted benzamides has been synthesized and evaluated for dopamine antagonist activity and for antagonism of cisplatin-induced emesis in the dog and in the ferret. It was found that modification of the 2-methoxy substituent of metoclopramide was detrimental to dopaminergic D2 antagonism but not necessarily to antagonism of cisplatin- induced emesis. A number of analogues having a@-keto,@-hydroxy,@-methoxy, &imino, ...