大环内酯类化合物的抗耐甲氧西林金黄色葡萄球菌活性研究进展  

Progress in the Study of Macrolide Hybrids with Antibacterial Potential Against Methicillin-resistant Staphylococcus aureus

作　　者：王俊 史玉敏 Wang Jun;Shi Yu-Min(School of Nuclear Technology and Chemical&Biology,Hubei University of Science and Technology,Xianning 437000)

机构地区：[1]湖北科技学院核技术与化学生物学院,咸宁437000

出　　处：《国外医药（抗生素分册）》2023年第5期306-313,共8页World Notes on Antibiotics

摘　　要：耐甲氧西林金黄色葡萄球菌(MRSA)是一种高度耐药和多重耐药致病菌,可引起严重感染甚至死亡。然而,目前可供选择的治疗MRSA感染药物屈指可数。大环内酯类抗生素对包括MRSA在内的多种致病菌具有广谱活性且具有安全性高和抗菌活性强等诸多优点。大环内酯与其他具有抗MRSA活性的药效团结合所得的杂合体可同时作用于MRSA的不同靶点,具有活性更强、药代动力学性质更优秀和毒副作用更低等特点。因此,合理设计大环内酯杂合体是获得新型抗MRSA药物候选物的有效途径。本文探讨了大环内酯杂合体的抗MRSA活性及构—效关系,为进一步研究提供参考。Methicillin-resistant Staphylococcus aureus(MRSA)is a highly resistant and multidrug-resistant pathogen that can lead to severe infections and even death.However,there are fairly limited treatment options for the treatment of MRSA infection.Macrolide antibiotics exhibit outstanding safety profiles,high efficacy,and broadspectrum activity against a range of infections,including MRSA.Macrolide hybrids,novel macrolide derivatives obtained through the combination of macrolide with other anti-MRSA pharmacophores,could act on different targets of MRSA simultaneously.Hence,macrolide hybrids usually endow with higher activity,better pharmacokinetic properties and lower side effects when compared with single part.Accordingly,reasonable design of macrolide hybrids is an effective approach to developing novel anti-MRSA candidates.In this paper,the anti-MRSA potential and the structure-activity relationship of macrolide hybrids are discussed,which will provide a reference for further research.

关 键 词：大环内酯 杂合体 抗菌 耐甲氧西林金葡菌 构—效关系 

分 类 号：R978.1[医药卫生—药品]