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一种新型1-氧杂头孢菌素与其他β-内酰胺类化合物的抗菌活性比较。

Antibacterial activity of a new 1-oxa cephalosporin compared with that of other beta-lactam compounds.

作者信息

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

出版信息

Antimicrob Agents Chemother. 1979 Aug;16(2):141-9. doi: 10.1128/AAC.16.2.141.

Abstract

The in vitro activity of (6R,7R)-7-{[carboxy(4-hydroxyphenyl)acetyl]amino}-7-methoxy-3-[[(1-methyl -1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-oxa-1-azabicyclo-[4.2.0]oct-2-ene -2-carboxylic acid was tested against isolates of gram-positive and negative bacteria and compared with those of cephalothin, cefuroxime, cefamandole, cefoxitin, cefotaxime, and carbenicillin. The compound was less active than the other compounds when tested against Staphylococcus aureus and Staphylococcus epidermidis. It had equal or slightly less activity than did cefotaxime when tested against members of the Enterobacteriaceae, but was 8- to 32-fold more active than the other cephalosporins against the Enterobacteriaceae, inhibiting most isolates at concentrations less than 0.5 mug/ml. The compound was twofold more active than cefotaxime and cefoxitin against Bacteroides, and it was twofold more active than cefotaxime and fourfold more active than carbenicillin against Pseudomonas aeruginosa. In vitro activity did not correlate with either the presence or type of beta-lactamase in either Enterobacteriaceae or Pseudomonas. The compound showed minimal synergy when combined with aminoglycosides or carbenicillin.

摘要

测试了(6R,7R)-7-{[羧基(4-羟基苯基)乙酰基]氨基}-7-甲氧基-3-[[(1-甲基-1H-四氮唑-5-基)硫代]甲基]-8-氧代-5-氧杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸对革兰氏阳性和阴性细菌分离株的体外活性,并与头孢噻吩、头孢呋辛、头孢孟多、头孢西丁、头孢噻肟和羧苄青霉素进行了比较。该化合物在针对金黄色葡萄球菌和表皮葡萄球菌进行测试时,活性低于其他化合物。在针对肠杆菌科成员进行测试时,其活性与头孢噻肟相当或略低,但对肠杆菌科的活性比其他头孢菌素高8至32倍,在浓度低于0.5μg/ml时能抑制大多数分离株。该化合物对拟杆菌的活性比头孢噻肟和头孢西丁高两倍,对铜绿假单胞菌的活性比头孢噻肟高两倍,比羧苄青霉素高四倍。体外活性与肠杆菌科或假单胞菌中β-内酰胺酶的存在或类型均无相关性。该化合物与氨基糖苷类或羧苄青霉素联合使用时显示出最小的协同作用。

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