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

被引：0

作者：

ODAKE, S

MORIKAWA, T

TSUCHIYA, M

IMAMURA, L

KOBASHI, K

机构：

[1] FUJI CHEM IND CO LTD, RES LABS 2, TAKAOKA, TOYAMA 933, JAPAN

[2] TOYAMA MED & PHARMACEUT UNIV, FAC PHARMACEUT SCI, TOYAMA 93001, JAPAN

来源：

BIOLOGICAL & PHARMACEUTICAL BULLETIN | 1994年 / 17卷 / 10期

关键词：

HELICOBACTER PYLORI UREASE; INHIBITION; HYDROXAMIC ACID; JACK BEAN UREASE;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 (I-50 values were near the order of 10(-6) M), and H-IIe-Gly-NHOH (I-50= 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.

引用

页码：1329 / 1332

页数：4

共 24 条

[1]

BLAKELEY RL, 1969, BIOCHEMISTRY-US, V8, P199

[2] RELATION OF CAMPYLOBACTER-PYLORIDIS TO GASTRITIS AND PEPTIC-ULCER [J].