European Journal of Medicinal Chemistry p. 847 - 868 (2018)
Update date:2022-08-15
Topics:
Aoki, Toshiaki
Yoshizawa, Hidenori
Yamawaki, Kenji
Yokoo, Katsuki
Sato, Jun
Hisakawa, Shinya
Hasegawa, Yasushi
Kusano, Hiroki
Sano, Masayuki
Sugimoto, Hideki
Nishitani, Yasuhiro
Sato, Takafumi
Tsuji, Masakatsu
Nakamura, Rio
Nishikawa, Toru
Yamano, Yoshinori
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.
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