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 hydroxamic acid (HXA) derivatives of aliphatic or aromatic carboxylic acids, amino acids and dipeptides. A number of HXAs potently inhibited the urease (I50 values were near the order of 10(-6)M), and H-Ile-Gly-NHOH (I50 = 0.20 x 10(-6)M) was the most potent inhibitor among the derivatives. HP urease was inhibited more potently, in general, than Jack bean (JB) urease by HXAs, and a correlation between the chemical structures of HXA derivatives and their inhibitory effects on HP urease was observed, in comparison with JB urease.
Odake
S
S
Research Laboratories II, Fuji Chemical Industries, Ltd., Toyama, Japan.
Morikawa
T
T
Tsuchiya
M
M
Imamura
L
L
Kobashi
K
K
D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D001555:Benzene Derivatives / Q000737:chemistry; D002417:Cattle; D003470:Culture Media; D016480:Helicobacter pylori / Q000187:drug effects / Q000201:enzymology*; D006877:Hydroxamic Acids / Q000378:metabolism / Q000494:pharmacology*; D010437:Peptic Ulcer / Q000201:enzymology / Q000382:microbiology; D013276:Stomach Ulcer / Q000201:enzymology / Q000382:microbiology; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000596:Amino Acids; D001555:Benzene Derivatives; D003470:Culture Media; D006877:Hydroxamic Acids; D014510:Urease