INHIBITION OF HELICOBACTER-PYLORI UREASE ACTIVITY BY HYDROXAMIC ACID-DERIVATIVES

Helicobacter pylori (HP) produces strong urease [EC 3.5.1.5], which is considered to play a role in the pathogenesis of gastritis and peptic ulcers. Inhibitions against this enzyme have been studied with hydrox amic acid (HXA) derivatives of aliphatic or aromatic carboxylic acids, amino acids and dipeptides. A number of HXAs potently inhibited the u rease (I-50 values were near the order of 10(-6) M), and H-IIe-Gly-NHO H (I-50= 0.20 x 10(-6) M) was the most potent inhibitor among the deri vatives. HP urease was inhibited more potently, in general, than Jack bean (JB) urease by HXAs, and a correlation between the chemical struc tures of HXA derivatives and their inhibitory effects on HP urease was observed, in comparison with JB urease.