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第四代头孢菌素的体外抗菌活性。

Antibacterial in vitro activity of fourth generation cephalosporins.

作者信息

Hancock R E, Bellido F

机构信息

Department of Microbiology and Immunology, University of British Columbia, Vancouver, Canada.

出版信息

J Chemother. 1996 Feb;8 Suppl 2:31-6.

PMID:8738844
Abstract

Cefpirome, cefepime and cefaclidine are distinguished by having a positively charged quaternary ammonium at carbon 3 of the dihydrothiazone ring. This confers the distinctive advantages of higher permeability across the outer membrane and low affinity for chromosomal cephalosporinases compared to the third generation cephalosporins which lack this quaternary ammonium moiety. These properties result in a marked advantage against resistant mutants of several species containing either derepressed class C chromosomal beta-lactamases or variant class A beta-lactamase. These unique properties have led to the suggestion that these compounds represent a "fourth generation" of cephalosporins.

摘要

头孢匹罗、头孢吡肟和头孢卡利定的特点是在二氢噻嗪环的3位碳原子上带有一个带正电荷的季铵基团。与缺乏该季铵部分的第三代头孢菌素相比,这赋予了它们在外膜上具有更高通透性以及对染色体头孢菌素酶低亲和力的独特优势。这些特性使得它们在对抗含有去阻遏C类染色体β-内酰胺酶或变异A类β-内酰胺酶的几种细菌的耐药突变体方面具有显著优势。这些独特的特性导致有人提出这些化合物代表了“第四代”头孢菌素。

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