Substituted 2-[(2-benzimidazolylsulfinyl) methyl] anilines as potential inhibitors of H+/K+ ATPase

GW Adelstein, CH Yen, RA Haack, S Yu…

Index: Adelstein, Gilbert W.; Yen, Chung H.; Haack, Richard A.; Yu, Stella; Gullikson, Gary; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1215 - 1220

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Citation Number: 23

Abstract

A series of substituted 2-[(2-benzimidazolylsulfinyl) methyl] anilines were synthesized as potential inhibitors of the acid secretory enzyme H+/K+ ATPase. Substitutions on the aniline nitrogen atom resulted in potent enzyme inhibition in vitro but weak activity in gastric fistula dogs. Electron-donating substituents on the aniline ring enhanced in vitro and in vivo potency relative to the unsubstituted analogue. The potency showed a correlation to the ...