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头孢甲肟对β-内酰胺酶的亲和力:一项分析

Affinity of cefmenoxime for beta-lactamases: an analysis.

作者信息

Labia R, Morand A, Verchere-Beaur C, Bryskier A

出版信息

Am J Med. 1984 Dec 21;77(6A):25-7. doi: 10.1016/s0002-9343(84)80070-4.

Abstract

The interactions of cefmenoxime with beta-lactamases in comparison with cefotaxime, moxalactam, cefoperazone, and ceftazidime have been determined. On-line computerized microacidimetry allowed determination of the affinity of these compounds with the enzymes, which was characterized by Km values. The beta-lactamases that were used were two cephalosporinases and one penicillinase. Within these data, the cephalosporins could be classified into three groups: (1) those with high affinity for the cephalosporinases and very poor affinity for the penicillinase (cefmenoxime, cefotaxime, and moxalactam); (2) those with moderate affinity for the cephalosporinases and very poor affinity for the penicillinase (ceftazidime); (3) those with poor affinity for all enzymes (cefoperazone). In the case of the penicillinase (TEM-1), only cefoperazone was subject to some hydrolysis.

摘要

已对头孢甲肟与β-内酰胺酶的相互作用进行了测定,并与头孢噻肟、拉氧头孢、头孢哌酮和头孢他啶作了比较。在线计算机化微量酸度测定法可测定这些化合物与酶的亲和力,其特征为米氏常数(Km值)。所使用的β-内酰胺酶为两种头孢菌素酶和一种青霉素酶。根据这些数据,头孢菌素可分为三组:(1)对头孢菌素酶具有高亲和力而对青霉素酶亲和力极差的(头孢甲肟、头孢噻肟和拉氧头孢);(2)对头孢菌素酶具有中等亲和力而对青霉素酶亲和力极差的(头孢他啶);(3)对所有酶亲和力均差的(头孢哌酮)。就青霉素酶(TEM-1)而言,只有头孢哌酮会发生一定程度的水解。

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