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哌嗪头孢菌素头孢哌酮的比较活性及β-内酰胺酶稳定性

Comparative activity and beta-lactamase stability of cefoperazone, a piperazine cephalosporin.

作者信息

Neu H C, Fu K P, Aswapokee N, Aswapokee P, Kung K

出版信息

Antimicrob Agents Chemother. 1979 Aug;16(2):150-7. doi: 10.1128/AAC.16.2.150.

Abstract

The in vitro activity and beta-lactamase stability of 7-[d(-)-alpha-(4-ethyl-2,3-dioxopiperazino-carbonylamino) -p-hydroxyphenylacetamido]-3-[(1-methyl)-5-tetrazolylthiomethyl] -Delta(3)-cephem-4-carboxylic acid (cefoperazone), a cephalosporin analog of piperacillin, were compared with the activities and stabilities of other cephalosporins and cephamycins. The compound was less active than cephalothin or cefamandole in inhibiting Staphylococcus aureus; it was as active as cefamandole and cefoxitin against most of the Enterobacteriaceae but less active than cefotaxime. It was more active than carbenicillin or piperacillin against Pseudomonas aeruginosa. In general, the compound was not active against Bacteroides. It was hydrolyzed by the beta-lactamases of some Escherichia coli which hydrolyzed cefamandole, but was stable to most plasmid-mediated, chromosomally mediated, inducible beta-lactamases in the Enterobacteriaceae and Pseudomonas.

摘要

7-[[d-(-)-α-(4-乙基-2,3-二氧代哌嗪甲酰氨基)-对羟基苯乙酰氨基]]-3-[(1-甲基)-5-四氮唑硫甲基]-Δ(3)-头孢烯-4-羧酸(头孢哌酮),一种哌拉西林的头孢菌素类似物,其体外活性及对β-内酰胺酶的稳定性与其他头孢菌素和头霉素的活性及稳定性进行了比较。该化合物在抑制金黄色葡萄球菌方面比头孢噻吩或头孢孟多活性低;在对抗大多数肠杆菌科细菌时,其活性与头孢孟多和头孢西丁相当,但比头孢噻肟活性低。在对抗铜绿假单胞菌方面,它比羧苄西林或哌拉西林活性高。总体而言,该化合物对拟杆菌无活性。它可被一些能水解头孢孟多的大肠杆菌的β-内酰胺酶水解,但对肠杆菌科和假单胞菌中大多数质粒介导、染色体介导的诱导型β-内酰胺酶稳定。

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