Antiulcer agents. 4-Substituted 2-guanidinothiazoles: reversible, competitive, and selective inhibitors of gastric H+, K+-ATPase

JL LaMattina, PA McCarthy, LA Reiter…

Index: LaMattina, John L.; McCarthy, Peter A.; Reiter, Lawrence A.; Holt, William F.; Yeh, Li-An Journal of Medicinal Chemistry, 1990 , vol. 33, # 2 p. 543 - 552

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Citation Number: 33

Abstract

A series of Csubstituted 2-guanidinothiazolea has been found to inhibit the gastric proton- pump enzyme H+, K+-ATPase. In general, these compounds were reversible inhibitors of canine gastric H+, K+-ATPase, competitive at the K+ site, and selective relative to canine renal Na+, K+-ATPase. Structure-activity relationship (SAR) studies on this series revealed no general replacement for the guanidinothiazole. On the other hand, use of pyrrolyl, ...