Journal of medicinal chemistry

Studies on histamine H2 receptor antagonists. 2. Synthesis and pharmacological activities of N-sulfamoyl and N-sulfonyl amidine derivatives

I Yanagisawa, Y Hirata, Y Ishii

Index: Yanagisawa, Isao; Hirata, Yasufumi; Ishii, Yoshio Journal of Medicinal Chemistry, 1987 , vol. 30, # 10 p. 1787 - 1793

Full Text: HTML

Citation Number: 44

Abstract

A series of N-sulfamoyl and N-sulfonyl amidines have been prepared and tested in vitro for Hz antihistamine activity on guinea pig atrium. In addition, several selected compounds were assessed as inhibitors of gastric acid secretion induced by histamine in anesthetized dogs. Structure-activity relationship studies showed that those compounds containing 2- [(diaminomethylene) amino] thiazole exhibited potent H2-receptor antagonist activity. ...