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Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship

2018; Elsevier BV; Volume: 155; Linguagem: Inglês

10.1016/j.ejmech.2018.06.014

1768-3254

Toshiaki Aoki, Hidenori Yoshizawa, Kenji Yamawaki, Katsuki Yokoo, Jun Sato, Shinya Hisakawa, Yasushi Hasegawa, Hiroki Kusano, Masayuki Sano, Hideki Sugimoto, Yasuhiro Nishitani, Takafumi Sato, Masakatsu Tsuji, Rio Nakamura, Toru Nishikawa, Yoshinori Yamano,

Antimicrobial Resistance in Staphylococcus

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.