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新型头孢菌素U-63196E的体外活性及β-内酰胺酶稳定性

In vitro activity and beta-lactamase stability of U-63196E, a novel cephalosporin.

作者信息

Neu H C, Labthavikul P

出版信息

Antimicrob Agents Chemother. 1983 Sep;24(3):375-82. doi: 10.1128/AAC.24.3.375.

DOI:10.1128/AAC.24.3.375
PMID:6605719
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC185328/
Abstract

The in vitro activity of U-63196E, a new broad-spectrum cephalosporin antibiotic, was studied against various gram-positive and gram-negative bacteria and compared with the in vitro activities of cefotaxime, moxalactam, cefoperazone, ceftazidime, and aztreonam. Although U-63196E inhibited many ampicillin-resistant bacteria and its activity against gram-negative species was similar to cefoperazone, it was much less active than the other agents. U-63196E was less active than cefazolin against gram-positive species, and it was less active than cefoxitin or moxalactam against Bacteroides fragilis. U-63196E did not inhibit most cefoperazone- or cefsulodin-resistant Pseudomonas aeruginosa. There was a difference between minimal inhibitory concentrations and minimal bactericidal concentrations for isolates which contained beta-lactamases. Plasmid beta-lactamases of the TEM, HSV, OXA, and PSE types hydrolyzed U-63196E. But U-63196E was relatively stable against hydrolysis by the chromosomal beta-lactamases.

摘要

研究了新型广谱头孢菌素抗生素U-63196E对各种革兰氏阳性菌和革兰氏阴性菌的体外活性,并与头孢噻肟、莫西沙星、头孢哌酮、头孢他啶和氨曲南的体外活性进行了比较。虽然U-63196E抑制了许多耐氨苄西林的细菌,且其对革兰氏阴性菌的活性与头孢哌酮相似,但它的活性比其他药物低得多。U-63196E对革兰氏阳性菌的活性低于头孢唑林,对脆弱拟杆菌的活性低于头孢西丁或莫西沙星。U-63196E不能抑制大多数耐头孢哌酮或头孢磺啶的铜绿假单胞菌。对于含有β-内酰胺酶的分离株,最小抑菌浓度和最小杀菌浓度之间存在差异。TEM、HSV、OXA和PSE型质粒β-内酰胺酶可水解U-63196E。但U-63196E对染色体β-内酰胺酶的水解相对稳定。

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本文引用的文献

1
The new beta-lactamase-stable cephalosporins.新型β-内酰胺酶稳定的头孢菌素。
Ann Intern Med. 1982 Sep;97(3):408-19. doi: 10.7326/0003-4819-97-3-408.
2
The beta-lactamases of gram-negative bacteria and their role in resistance to beta-lactam antibiotics.革兰氏阴性菌的β-内酰胺酶及其在对β-内酰胺类抗生素耐药性中的作用。
J Antimicrob Chemother. 1976 Jun;2(2):115-57. doi: 10.1093/jac/2.2.115.
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The comparative beta-lactamase resistance and inhibitory activity of 1-oxa cephalosporin, cefoxitin and cefotaxime.1-氧杂头孢菌素、头孢西丁和头孢噻肟的β-内酰胺酶耐药性及抑制活性比较
J Antibiot (Tokyo). 1979 Sep;32(9):909-14. doi: 10.7164/antibiotics.32.909.
4
Comparative activity and beta-lactamase stability of cefoperazone, a piperazine cephalosporin.哌嗪头孢菌素头孢哌酮的比较活性及β-内酰胺酶稳定性
Antimicrob Agents Chemother. 1979 Aug;16(2):150-7. doi: 10.1128/AAC.16.2.150.