In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria.
In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria.
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DOI：
10.1128/aac.01454-17
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发表时间：
2018-01
影响因子：
4.9
通讯作者：
Yamano Y
中科院分区：
文献类型：
--
作者：
Ito A;Sato T;Ota M;Takemura M;Nishikawa T;Toba S;Kohira N;Miyagawa S;Ishibashi N;Matsumoto S;Nakamura R;Tsuji M;Yamano Y
Cefiderocol（CFDC; S-649266）是一种新型肠外铁载体头孢菌素，与儿茶酚部分结合，具有特征性抗菌谱，对广泛的需氧革兰氏阴性细菌种属具有强效活性，包括肠杆菌科的碳青霉烯类耐药菌株和非发酵细菌，如铜绿假单胞菌和鲍曼不动杆菌。头孢地罗可主要对肠杆菌科和非发酵菌的青霉素结合蛋白3（PBP 3）具有与头孢他啶相似的亲和力。铜绿假单胞菌中铁转运蛋白PiuA或大肠杆菌中CirA和Fiu两者的缺乏导致头孢地罗可MIC增加16倍，表明这些铁转运蛋白有助于头孢地罗可穿过外膜。肺炎克雷伯氏菌OmpK 35/36缺陷和铜绿假单胞菌外排泵MexA-MexB-OprM过量产生对头孢地罗可活性无显著影响。
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 Enterobacteriaceae and nonfermenting bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii. Cefiderocol has affinity mainly for penicillin-binding protein 3 (PBP3) of Enterobacteriaceae and nonfermenting bacteria similar to that of ceftazidime. A deficiency of the iron transporter PiuA in P. aeruginosa or both CirA and Fiu in Escherichia coli 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 Klebsiella pneumoniae and the overproduction of efflux pump MexA-MexB-OprM in P. aeruginosa showed no significant impact on the activity of cefiderocol.