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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

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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

Toshiaki Aoki et al. Eur J Med Chem.

Abstract

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.

Keywords: Cefiderocol; Multi-drug resistant Gram-negative pathogens; Siderophore; Siderophore cephalosporin.

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