Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., 1-1, Futabacho, 3-chome, Toyonaka, 561-0825, Osaka, Japan.
Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd., 1-1, Futabacho, 3-chome, Toyonaka, 561-0825, Osaka, Japan.
Eur J Med Chem. 2018 Jul 15;155:847-868. doi: 10.1016/j.ejmech.2018.06.014. Epub 2018 Jun 8.
The structure-activity relationship (SAR) for a novel series of catechol conjugated siderophore cephalosporins is described with their in vitro activities against multi-drug resistant Gram-negative pathogens including Pseudomonas aeruginosa, Acinetobacter baumannii, Stenotrophomonas maltophilia and Enterobacteriaceae. Cefiderocol (3) was one of the best molecules which displayed well-balanced and potent activities against multi-drug resistant Gram-negative pathogens including carbapenem resistant bacteria among the prepared compounds with the modified C-7 side chain and the modified C-3 side chain. Cefiderocol (3) is a highly promising parenteral cephalosporin for the treatment of multi-drug resistant Gram-negative infection.
描述了一系列新型儿茶酚共轭头孢菌素类化合物的构效关系（SAR），并测试了它们对包括铜绿假单胞菌、鲍曼不动杆菌、嗜麦芽窄食单胞菌和肠杆菌科在内的多种耐药革兰氏阴性病原体的体外活性。头孢他啶（3）是其中最好的分子之一，与其他经过修饰的 C-7 侧链和 C-3 侧链的化合物相比，它对包括耐碳青霉烯类细菌在内的多种耐药革兰氏阴性病原体具有良好的平衡和强大的活性。头孢他啶（3）是一种很有前途的治疗多重耐药革兰氏阴性感染的新型注射用头孢菌素。
