Structure-Activity Relationship of Omeprazole and Analogs as Helicobacter pylori Urease Inhibitors

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...

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Veröffentlicht in:	Journal of medicinal chemistry 1995-12, Vol.38 (25), p.4906-4916
Hauptverfasser:	Kuehler, Thomas C, Fryklund, Jan, Bergman, Nils-ke, Weilitz, Jessica, Lee, Adrian, Larsson, Haakan
Format:	Artikel
Sprache:	eng
Schlagworte:	Ammonia - metabolism Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Anti-Ulcer Agents - chemical synthesis Anti-Ulcer Agents - chemistry Anti-Ulcer Agents - pharmacology Benzamides - pharmacology Binding Sites - drug effects Biological and medical sciences Cysteine - drug effects Digestive system Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Helicobacter pylori Helicobacter pylori - drug effects Helicobacter pylori - enzymology Hydrogen-Ion Concentration Medical sciences Mercaptoethanol - pharmacology Mice Mice, Inbred Strains Omeprazole - analogs & derivatives Omeprazole - chemical synthesis Omeprazole - pharmacology Pharmacology. Drug treatments Structure-Activity Relationship Urease - antagonists & inhibitors Urease - metabolism
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