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

MF Hibert, R Hoffmann, RC Miller…

Index: Hibert; Hoffmann; Miller; Carr Journal of Medicinal Chemistry, 1990 , vol. 33, # 6 p. 1594 - 1600

Full Text: HTML

Citation Number: 130

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.