2.B.112. The Quinoline Thiourea-based Zinc Ionophore (QT-ZnI) Family
Perturbation of ion homeostasis is a potential therapeutic strategy to fight against antibacterial resistance and other channelopathies. Dey et al. 2023 reported the development of 8-aminoquinoline (QN) derivatives and their transmembrane Zn2+ transport activities. Potent QN-based Zn2+ transporters exhibit antibacterial properties against Gram-positive bacteria with reduced hemolytic activity and cytotoxicity to mammalian cells. They showed in vivo efficacy against Staphylococcus aureus, prevented bacterial resistance, and restored susceptibility of gentamicin and methicillin-resistant S. aureus to commercially available beta-lactams and other antibiotics that had lost their activity against the drug-resistant bacterial strain (Dey et al. 2023). Several QN derivatives were tested for Zn2+ transport activity, and several proved effective. The mechanism may involve Zn2+:H+ antiport.