Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site

Abstract

A conformation-activity relationship study of 5-HT3 receptor antagonists was used to define a pharmacophore and receptor map to qualitatively account for their activity. The design and synthesis of specific keto-amino-indole derivatives that are potent 5-HT3 receptor antagonists gave some support to the model.