WuXi AppTec (Wuhan), Hubei, PR China.
Key Laboratory of Drug Prevention and Control Technology of Zhejiang Province, Zhejiang Police College, Hangzhou, PR China.
Eur J Med Chem. 2018 Sep 5;157:1081-1095. doi: 10.1016/j.ejmech.2018.08.061. Epub 2018 Aug 27.
Methicillin-resistant Staphylococcus aureus (MRSA) is the most common pathogen both in hospital and community settings, and is capable of causing serious and even fatal infections. Several antibiotics have been approved for the treatment of infections caused by MRSA, but MRSA has already developed resistance to them. More than ever, it's imperative to develop novel, high effective and fast acting anti-MRSA agents. Quinolones are one of the most common antibiotics in clinical practice used to treat various bacterial infections, and some of them displayed excellent in vitro and in vivo anti-MRSA activities, so quinolone derivatives are one of the most promising candidates. This review summarizes the recent developments of quinolone derivatives with potential activity against MRSA, and the structure-activity relationship is also discussed.
耐甲氧西林金黄色葡萄球菌（MRSA）是医院和社区环境中最常见的病原体，能够引起严重甚至致命的感染。有几种抗生素已被批准用于治疗由 MRSA 引起的感染，但 MRSA 已经对这些抗生素产生了耐药性。比以往任何时候都更需要开发新型、高效和快速作用的抗 MRSA 药物。喹诺酮类是临床实践中最常用的抗生素之一，用于治疗各种细菌感染，其中一些具有出色的体外和体内抗 MRSA 活性，因此喹诺酮类衍生物是最有前途的候选药物之一。本综述总结了具有抗 MRSA 活性的喹诺酮类衍生物的最新研究进展，并讨论了它们的构效关系。
