Department of Chemistry, University of Manitoba, Winnipeg, MB, Canada.
Department of Medical Microbiology and Infectious Diseases, University of Manitoba, Winnipeg, MB, Canada.
ChemMedChem. 2024 Aug 1;19(15):e202400175. doi: 10.1002/cmdc.202400175. Epub 2024 Jun 15.
Multicomponent therapy combining antibiotics with enhancer molecules known as adjuvants is an emerging strategy to combat antimicrobial resistance. Niclosamide is a clinically relevant anthelmintic drug with potential to be repurposed for its inherent antibacterial activity against Gram-positive bacteria and its ability to potentiate the antibacterial activity of colistin against susceptible and resistant Gram-negative bacteria. Herein, sulfonamide analogs of niclosamide were prepared and found to enhance colistin activity against Gram-negative bacteria. The ability of niclosamide and the new sulfonamide analogs to synergize with bacitracin against vancomycin-resistant Enterococcus faecium was also discovered.
联合抗生素和增强分子（称为佐剂）的多组分疗法是一种应对抗微生物药物耐药性的新兴策略。尼氯硝唑是一种具有临床相关性的驱虫药物，具有固有抗革兰氏阳性菌活性和增强黏菌素对敏感和耐药革兰氏阴性菌的抗菌活性的潜力，可被重新用于治疗。本文制备了尼氯硝唑的磺胺类似物，并发现它们能够增强黏菌素对革兰氏阴性菌的活性。还发现尼氯硝唑和新的磺胺类似物能够与杆菌肽协同作用，抑制万古霉素耐药粪肠球菌。
