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L-658,310,一种新型注射用头孢菌素。I. 体外抗菌特性。

L-658,310, a new injectable cephalosporin. I. In vitro antibacterial properties.

作者信息

Weissberger B A, Abruzzo G K, Fromtling R A, Gill C, Ponticas S, Valiant M E, Shungu D L, Gadebusch H H

机构信息

Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065-0900.

出版信息

J Antibiot (Tokyo). 1989 May;42(5):795-806. doi: 10.7164/antibiotics.42.795.

Abstract

The in vitro antibacterial spectrum of L-658,310, a new semisynthetic cephalosporin, was compared with ceftazidime, aztreonam and piperacillin against a wide variety of randomly selected human clinical isolates. The compound was found to be a broad spectrum bactericidal agent that was more potent than any of the comparison drugs against glucose nonfermenting bacteria. It has especially potent activity against Pseudomonas aeruginosa including multiply-resistant strains. The superior activity of L-658,310 against this group of organisms is attributed to the presence of the dihydroxy substituents on the 2-methylisoindoline moiety of the compound. L-658,310 is not cross-resistant with either imipenem, ceftazidime or piperacillin (representatives of three different classes of beta-lactam compounds) against P. aeruginosa. The lack of cross-resistance with ceftazidime extends to other glucose nonfermenters and several strains of Enterobacteriaceae as well. The compound is active against bacteria known to possess either R-plasmid- or chromosomally-mediated beta-lactamases.

摘要

将一种新型半合成头孢菌素L-658,310的体外抗菌谱与头孢他啶、氨曲南和哌拉西林针对多种随机选择的人类临床分离株进行了比较。发现该化合物是一种广谱杀菌剂,对葡萄糖非发酵菌的效力比任何一种对照药物都更强。它对铜绿假单胞菌具有特别强的活性,包括多重耐药菌株。L-658,310对这组生物体的优越活性归因于该化合物2-甲基异吲哚啉部分上存在二羟基取代基。L-658,310与亚胺培南、头孢他啶或哌拉西林(三种不同类别的β-内酰胺化合物的代表)对铜绿假单胞菌不存在交叉耐药性。与头孢他啶缺乏交叉耐药性也延伸至其他葡萄糖非发酵菌和几株肠杆菌科细菌。该化合物对已知具有R质粒或染色体介导的β-内酰胺酶的细菌具有活性。

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