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J Antibiot (Tokyo) ; 77(5): 331-333, 2024 May.
Article in English | MEDLINE | ID: mdl-38467778

ABSTRACT

The emergence and spread of antimicrobial resistance are global threats. Pseudomonas aeruginosa (P. aeruginosa) is responsible for a substantial proportion of this global health issue because of its intrinsic resistance to many antibiotics due to the impermeability of its outer membrane and its multidrug efflux pump systems. Therefore, therapeutic drugs are limited, and the development of new drugs is extremely challenging. As an alternative approach, we focused on a combinational treatment strategy and found that 5-O-mycaminosyltylonolide (OMT) showed potent antibacterial activity against P. aeruginosa in the presence of an efflux pump inhibitor, phenylalanine-arginine beta-naphthylamide (PAßN). In this report, we prepared a PAßN derivative and compared the potentiation activity of OMT by PAßNs against multidrug-resistant P. aeruginosa clinical isolates.


Subject(s)
Anti-Bacterial Agents , Dipeptides , Drug Resistance, Multiple, Bacterial , Microbial Sensitivity Tests , Pseudomonas aeruginosa , Tylosin/analogs & derivatives , Pseudomonas aeruginosa/drug effects , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Drug Resistance, Multiple, Bacterial/drug effects , Dipeptides/pharmacology , Dipeptides/chemistry , Drug Synergism , Humans
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