- 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
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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.
- 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
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p. 847 - 868
(2018/07/03)
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- CEPHALOSPORIN HAVING CATECHOL GROUP
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The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
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Page/Page column 61-62
(2011/07/30)
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