N-sulfonyloxy-β-lactam inhibitors for β-lactamases

被引：22

作者：

Bulychev, A

Bellettini, JR

O'Brien, M

Crocker, PJ

Samama, JP

Miller, MJ

Mobashery, S ^{[1
]}

机构：

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

[2] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA

[3] CNRS, Inst Pharmacol & Biol Struct, Grp Cristallog Biol, F-31077 Toulouse, France

来源：

TETRAHEDRON | 2000年 / 56卷 / 31期

关键词：

beta-lactamase; inhibition;

D O I：

10.1016/S0040-4020(00)00427-0

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Structure-function analysis with a series of N-sulfonyloxy beta-lactam molecules as inhibitors of beta-lactamases is reported. The best of these compounds acylate the active site of the class A TEM-1 beta-lactamase from Escherichia coli rapidly, and resist deacylation. Whereas acylation of the active site of the class C beta-lactamase from Enterobacter cloacae was not seen, these compounds function as competitive inhibitors of this enzyme. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：5719 / 5728

页数：10

共 37 条

[1]

[Anonymous], 1996, WORLD HLTH REP

[2]

[Anonymous], 1992, EMERGING INFECT MICR

[3]

BELAAOUAJ A, 1994, FEMS MICROBIOL LETT, V120, P75

[4] C-ACYLATION UNDER VIRTUALLY NEUTRAL CONDITIONS [J].