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头孢地尔的抗菌特性,一种新型的铁载体头孢菌素,针对革兰氏阴性菌。

Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria.

机构信息

Shionogi & Co., Ltd., Toyonaka, Osaka, Japan

Shionogi & Co., Ltd., Toyonaka, Osaka, Japan.

出版信息

Antimicrob Agents Chemother. 2017 Dec 21;62(1). doi: 10.1128/AAC.01454-17. Print 2018 Jan.

Abstract

Cefiderocol (CFDC; S-649266), a novel parenteral siderophore cephalosporin conjugated with a catechol moiety, has a characteristic antibacterial spectrum with a potent activity against a broad range of aerobic Gram-negative bacterial species, including carbapenem-resistant strains of and nonfermenting bacteria such as and Cefiderocol has affinity mainly for penicillin-binding protein 3 (PBP3) of and nonfermenting bacteria similar to that of ceftazidime. A deficiency of the iron transporter PiuA in or both CirA and Fiu in caused 16-fold increases in cefiderocol MICs, suggesting that these iron transporters contribute to the permeation of cefiderocol across the outer membrane. The deficiency of OmpK35/36 in and the overproduction of efflux pump MexA-MexB-OprM in showed no significant impact on the activity of cefiderocol.

摘要

头孢地尔(CFDC;S-649266)是一种新型的注射用铁载体头孢菌素,与儿茶酚部分偶联,具有广谱抗菌谱,对多种需氧革兰氏阴性菌具有强大的活性,包括耐碳青霉烯类的 和非发酵菌,如 。头孢地尔主要与 青霉素结合蛋白 3(PBP3)和非发酵菌的亲和力类似于头孢他啶。 的铁转运蛋白 PiuA 或 的 CirA 和 Fiu 缺失导致头孢地尔 MIC 增加 16 倍,表明这些铁转运蛋白有助于头孢地尔穿过外膜的渗透。 的 OmpK35/36 缺失和 的外排泵 MexA-MexB-OprM 过度表达对头孢地尔的活性没有显著影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5246/5740388/bb73c7911536/zac0011867790001.jpg

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