Structure-activity relationship of omeprazole and analogs as Helicobacter pylori urease inhibitors

…, J Fryklund, N Bergman, J Weilitz, A Lee…

Index: Kuhler; Fryklund; Bergman; Weilitz; Lee; Larsson Journal of Medicinal Chemistry, 1995 ,  vol. 38,  # 25  p. 4906 - 4916

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Citation Number: 83

Abstract

Helicobacter pylori urease belongs to a family of highly conserved urea-hydrolyzing enzymes. A common feature of these enzymes is the presence of two Lewis acid nickel ions and a reactive cysteine residue in the active site. The H+/K+-ATPase inhibitor omeprazole is a prodrug of a sulfenamide which covalently modifies cysteine residues on the luminal side of the H+/K+-ATPase of gastric parietal cells. Omeprazole and eight analogues were ...