(H+, K+)-ATPase inhibiting 2-[(2-pyridylmethyl) sulfinyl] benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The …

…, J Senn-Bilfinger, WA Simon, U Krueger…

Index: Kohl; Sturm; Senn-Bilfinger; Simon; Kruger; Schaefer; Rainer; Figala; Klemm Journal of Medicinal Chemistry, 1992 , vol. 35, # 6 p. 1049 - 1057

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Citation Number: 77

Abstract

[(Pyridylmethyl) sulf'iiyl] benzimidazoles 1 (PSBs) are a class of highly potent antisecretory (H+, K+)-ATPase inhibitors which need to be activated by acid to form their active principle, the cyclic sulfenamide 4. Selective inhibitors of the (H+, K+)-ATPase in vivo give rise to the nonselective thiophile 4 solely at low pH, thus avoiding interaction with other thiol groups in the body. The propensity to undergo the acid-catalyzed transformation is dependent on ...