Quinoline Thiourea-Based Zinc Ionophores with Antibacterial Activity.
Journal of medicinal chemistry(2023)
摘要
The increasing resistance of bacteria to commercially available antibiotics threatens patient safety in healthcare settings. Perturbation of ion homeostasis has emerged as a potential therapeutic strategy to fight against antibacterial resistance and other channelopathies. This study reports the development of 8-aminoquinoline (QN) derivatives and their transmembrane Zn transport activities. Our findings showed that a potent QN-based Zn transporter exhibits promising antibacterial properties against Gram-positive bacteria with reduced hemolytic activity and cytotoxicity to mammalian cells. Furthermore, this combination showed excellent in vivo efficacy against . Interestingly, this combination prevented bacterial resistance and restored susceptibility of gentamicin and methicillin-resistant to commercially available β-lactam and other antibiotics that had lost their activity against the drug-resistant bacterial strain. Our findings suggest that the transmembrane transport of Zn by QN derivatives could be a promising strategy to combat bacterial infections and restore the activity of other antibiotics.
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关键词
antibacterial activity,zinc,thiourea-based
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