Studies on (H+-K+)-ATPase inhibitors of gastric acid secretion. Prodrugs of 2-[(2-pyridinylmethyl) sulfinyl] benzimidazole proton-pump inhibitors

JC Sih, W bin Im, A Robert, DR Graber…

Index: Sih, John C.; Im, Wha Bin; Robert, Andre; Graber, David R.; Blakeman, David P. Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1049 - 1062

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Citation Number: 35

Abstract

The synthesis of N-substituted benzimidazole (H+-K+)-ATPase or proton-pump inhibitors is described. These compounds were prepared to function as prodrugs of the parent NH compound and evaluated for their ability to inhibit gastric (H+-K+)-ATPase and gastric acid secretion. The prodrugs reported rely on either in vivo esterase hydrolysis for liberation of the parent compound (type I and type 11) or require an acid environment for release of the ...