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头孢甲肟对β-内酰胺酶的作用

Behaviour of cefmenoxime towards beta-lactamases.

作者信息

Labia R, Morand A, Ben Yaghlane H, Bryskier A

出版信息

Drugs Exp Clin Res. 1985;11(6):373-8.

PMID:3939122
Abstract

Using several well-characterized beta-lactamases isolated from Gram-negative bacteria, the interactions of cefmenoxime, a new methoxy-imino-amino-2-thiazol cephalosporin were compared with those of cefotaxime, lamoxactam, cefoperazone and ceftazidime. On-line computerized microacidimetry allowed determination of the affinity of these compounds for the enzymes, which was characterized by Ki values. Microacidimetry showed poor interactions of cefmenoxime with penicillinase TEM-1 (low Vm, poor affinity) whereas it showed a high affinity for the cephalosporinases, as is also the case for cefotaxime or lamoxactam. Both cefmenoxime and cefotaxime showed relative susceptibility in Masuda's double disc technique.

摘要

使用从革兰氏阴性菌中分离出的几种特性明确的β-内酰胺酶,将新型甲氧基-亚氨基-氨基-2-噻唑头孢菌素头孢甲肟与头孢噻肟、拉氧头孢、头孢哌酮和头孢他啶的相互作用进行了比较。在线计算机化微量酸量滴定法可测定这些化合物与酶的亲和力,其特征为抑制常数(Ki)值。微量酸量滴定法显示头孢甲肟与青霉素酶TEM-1的相互作用较弱(最大反应速度低、亲和力差),而它对头孢菌素酶具有高亲和力,头孢噻肟或拉氧头孢也是如此。在增田双纸片法中,头孢甲肟和头孢噻肟均表现出相对敏感性。

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