Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding

F Heidempergher, A Pillan, V Pinciroli…

Index: Heidempergher, Franco; Pillan, Antonio; Pinciroli, Vittorio; Vaghi, Fabrizio; Arrigoni, Claudio; Bolis, Giorgio; Caccia, Carla; Dho, Luciano; McArthur, Robert; Varasi, Mario Journal of Medicinal Chemistry, 1997 , vol. 40, # 21 p. 3369 - 3380

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Citation Number: 31

Abstract

A possible bioisosterism between the benzamido and the phenylimidazolidin-2-one moieties has been suggested on the basis of the similarity between the molecular electrostatic potential (MEP) of metoclopramide, a D2 receptor antagonist with weak 5-HT3 receptor antagonist properties, and zetidoline, a D2 receptor antagonist. Starting from this premise, a series of phenylimidazolidin-2-one derivatives bearing a basic azabicycloalkyl ...