含有1,2,3-三氮唑结构片段的杂合体的抗耐药金葡菌活性研究进展  

Research progress in 1,2,3-triazole-containing hybrids with antibacterial activities against drug-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,China)

机构地区：[1]湖北科技学院核技术与化学生物学院,湖北咸宁437000

出　　处：《中国药物化学杂志》2023年第5期386-396,共11页Chinese Journal of Medicinal Chemistry

摘　　要：耐药金葡菌尤其是耐甲氧西林金葡菌是院内及社区感染的主要元凶,可引起局部脓肿、腹泻、肺部感染、泌尿系统感染及烫伤创伤表面感染等。耐甲氧西林金葡菌具有广谱耐药性,临床上可供选择的药物屈指可数。因此,亟需开发新型抗耐药金葡菌尤其是抗耐甲氧西林金葡菌药物。1,2,3-三氮唑易于合成,可与多个药物靶点通过非共价键结合,既是药物分子中常见的药效团,也可作为连接子连接不同的药效团。近年来,药物化学家将1,2,3-三氮唑与其他抗耐药金葡菌药效团杂合,或以1,2,3-三氮唑为连接子将其他不同的抗耐甲氧西林金葡菌药效团连接在一起,发现了多个具有优秀抗耐药金葡菌活性的含有1,2,3-三氮唑结构片段的杂合体。本文作者就自2018年以来报道的具有抗耐药金葡菌活性的含有1,2,3-三氮唑结构片段的杂合体的研究进展进行综述,并探讨其构效关系,以期为相关领域的研究提供参考。Drug-resistant Staphylococcus aureus especially methicillin-resistant S.aureus,as the main culprit of hospital and community infections,can cause local abscess,diarrhea,lung infection,urinary system infection and scald wound surface infection.Methicillin-resistant S.aureus demonstrated a broad spectrum of drug resistance,and the current available drugs are numbered.Therefore,it is urgent to develop new anti-drug-resistant S.aureus especially anti-methicillin-resistant S.aureus drugs.1,2,3-Triazole can be constructed effectively by click chemistry and can act on multiple drug targets through non-covalent bonds.Notably,1,2,3-triazole is a common pharmacophore in drug molecules,but also can link different pharmacophores as a linker.In recent years,medicinal chemists have found a number of 1,2,3-triazole-containing hybrid with excellent anti-drug-resistant S.aureus activities by hybridizing 1,2,3-triazole with other anti-drug-resistant S.aureus pharmacophores,or connecting 1,2,3-triazole with other anti-drug-resistant S.aureus pharmacophores.In this paper,the latest research progress regarding 1,2,3-triazole-containing hybrids with anti-drug-resistant S.aureus activities developed since 2018 was reviewed,and the structure-activity relationships were summarized,in order to provide references for the future research in related fields.Notably,hybrids 9b and 10a possessed promising in vivo and in vitro antibacterial efficacies,and merited further evaluations.

关 键 词：1 2 3-三氮唑 杂合体 抗菌 耐药 耐甲氧西林金葡菌 构效关系 

分 类 号：R914[医药卫生—药物化学]