Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, China.
Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, China.
Eur J Med Chem. 2023 Nov 5;259:115689. doi: 10.1016/j.ejmech.2023.115689. Epub 2023 Jul 29.
In recent years, the overuse of antibiotics has resulted in the emergence of antibiotic resistance, which is a serious global health problem. Methicillin-resistant Staphylococcus aureus (MRSA) is a common and virulent bacterium in clinical practice. Numerous researchers have focused on developing new candidate drugs that are effective, less toxic, and can overcome MRSA resistance. Thiazole derivatives have been found to exhibit antibacterial activity against drug-sensitive and drug-resistant pathogens. By hybridizing thiazole with other antibacterial pharmacophores, it is possible to obtain more effective antibacterial candidate drugs. Thiazole derivatives have shown potential in developing new drugs that can overcome drug resistance, reduce toxicity, and improve pharmacokinetic characteristics. This article reviews the recent progress of thiazole compounds as potential antibacterial compounds and examines the structure-activity relationship (SAR) in various directions. It covers articles published from 2018 to 2023, providing a comprehensive platform to plan and develop new thiazole-based small MRSA growth inhibitors with minimal side effects.
近年来,抗生素的过度使用导致了抗生素耐药性的出现,这是一个严重的全球健康问题。耐甲氧西林金黄色葡萄球菌(MRSA)是临床实践中常见且具有毒性的细菌。许多研究人员专注于开发新的候选药物,这些药物具有疗效好、毒性低、能克服 MRSA 耐药性的特点。噻唑衍生物已被发现对药敏和耐药病原体具有抗菌活性。通过将噻唑与其他抗菌药效团杂交,可以获得更有效的抗菌候选药物。噻唑衍生物在开发新的能够克服耐药性、降低毒性和改善药代动力学特性的药物方面显示出了潜力。本文综述了噻唑类化合物作为潜在抗菌化合物的最新进展,并从各个方向探讨了结构-活性关系(SAR)。涵盖了 2018 年至 2023 年发表的文章,为计划和开发具有最小副作用的新型基于噻唑的小剂量 MRSA 生长抑制剂提供了一个全面的平台。