Inhibition of β-lactamases by 6,6-bis(hydroxylmethyl) penicillanate

被引：4

作者：

Nagase, T

Golemi, D

Ishiwata, A

Mobashery, S ^{[1
]}

机构：

[1] Wayne State Univ, Inst Drug Design, Detroit, MI 48202 USA

[2] Wayne State Univ, Dept Chem, Detroit, MI 48202 USA

来源：

BIOORGANIC CHEMISTRY | 2001年 / 29卷 / 03期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1006/bioo.2001.1205

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

beta -Lactamases of classes A and C are the two most prevalent resistant determinants to beta -lactam antibiotics among bacterial pathogens. Both these enzymes pursue different mechanisms For their catalytic processes, highlighted by the fact that the hydrolytic water molecule in each approaches the ester of the intermediary acyl-enzyme species from the opposite ends. 6,6Bis(hydroxylmethyl)penicillanate was designed as an inhibitor that would impair the approach of the hydrolytic water molecule in either of these enzymes upon formation of the acyl-enzyme species. The design, synthesis, and kinetic evaluation of this inhibitor are disclosed herein. (C) 2001 Academic Press.

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收藏

页码：140 / 145

页数：6

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