抗MRSA咪唑杂合体的研究进展  

Recent Progress in Imidazole Hybrids with Antibacterial Potential against Methicillin-resistant Staphylococcus aureus

作　　者：邓军 邓吉聪 李新丹 吴建辉 付瑶 关伟业 Deng Jun;Deng Ji-cong;Li Xin-dan;Wu Jian-hui;Fu Yao;Guan Wei-ye(Guangdong Zhongsheng Pharmaceutical Co.,Ltd.,Dongguan 523320;Guangdong Xianqiang Pharmaceutical Co.,Ltd.,Guangzhou 510900)

机构地区：[1]广东众生药业股份有限公司,东莞523320 [2]广东先强药业有限公司,广州510900

出　　处：《国外医药（抗生素分册）》2021年第6期339-345,共7页World Notes on Antibiotics

摘　　要：耐甲氧西林金黄色葡萄球菌(MRSA)是一种流行范围广、致病力强、发病率和病死率高的病原菌,可引起局部脓肿、呼吸道感染、腹泻和泌尿系统感染甚至死亡。MRSA的生物膜保护作用和迅速产生耐药性的特性,使得MRSA的治疗异常棘手。因此,亟需开发新型抗MRSA药物。杂合策略是开发新药常用手段,目前多个杂合体药物已用于临床或处于临床评价阶段。咪唑类化合物具有潜在的抗菌活性,将咪唑与其他具有抗菌活性的药效团杂合可能会获得对包括MRSA在内的多种致病菌具有良好广谱抗菌活性的候选化合物。本文将介绍自2011年以来发展的具有抗MRSA活性的咪唑杂合体的最新研究进展,并探讨构-效关系,为今后进一步开发活性更高的候选物提供参考。Methicillin-resistant Staphylococcus aureus (MRSA),one of the major pathogens with high virulence,high morbidity and mortality,can cause local abscess,respiratory tract infection,diarrhea,urinary tract infection and even death.Treatment of MRSA infections is challenging which is mainly attributed to the rapidly evolving resistance mechanisms combined with the protective biofilms of S.aureus,creating an urgent demand to develop novel anti-MRSA agents.Hybridization is one of the most common strategies to develop new drugs,and currently,several hybrids have already been applied in clinic or under clinical evaluations.Imidazole derivatives possess potential antibacterial activity,and hybridization of imidazole pharmacophore with other antibacterial pharmacophores into one molecule may provide novel antibacterial candidates with broad-spectrum activity against various pathogens,including MRSA.This review is an endeavor to highlight the current scenario of imidazole hybrids with potential anti-MRSA activity,and structure-activity relationships are also discussed,covering articles published between 2011 and 2021.

关 键 词：咪唑 杂合体 耐甲氧西林金黄色葡萄球菌 构-效关系 

分 类 号：R978.1[医药卫生—药品]