H⁺/K⁺-ATPase Inhibitors

Abstract

Gastric H⁺/K⁺-ATPase, located in the parietal cell, is responsible for the final step of acid secretion in the stomach. Since omeprazole, a sulfinyl compound, was found to inhibit H⁺/K⁺-ATPase in 1983, there has been considerable interest in H⁺/K⁺-ATPase inhibitor as a splendid drug for the treatment of peptic ulcer. H⁺/K⁺-ATPase inhibitors are classified into two categories. One is an irreversible inhibitor binding to a critical thiol group on the enzyme, such as omeprazole, lansoprazole and NC-1300-O-3, and the other is a reversible K⁺-competitive inhibitor. In the former, substituted pyridyl derivatives transform in the acid compartments of the parietal cell into the active inhibitor. This paper reviews the development of H⁺/K⁺-ATPase inhibitors.