二氢吲哚-2,3-二酮衍生物抑菌活性研究进展谭画元1张广龙1吉礼涛1王钦1卢奕朵1欧阳贵平1王贞超1,2,3*李洙锐1,2*(1贵州大学药学院;2贵州大学绿色农药与农业生物工程教育部重点实验室;3贵州省合成药物工程实验室贵阳550025)*联系人,王贞超E-mail:wzc.4884@163.com;李洙锐E-mail:li-zhurui@163.com国家自然科学基金项目(21867004,22007022)、贵州省科技计划平台项目(黔科合平台人才20185781)和贵州省科技计划项目(黔科合基础-ZZK[2021]重点034)资助2022-07-29收稿,2022-09-15接受摘要二氢吲哚-2,3-二酮是一种结构简单且应用广泛的药物小分子,其衍生物的合成、结构和药理活性等备受关注。已有报道表明二氢吲哚-2,3-二酮具有抗菌、抗衰老、降血脂、抗癫痫、抗病毒等多种生物活性。本文主要围绕抑菌生物活性,对国内外关于二氢吲哚-2,3-二酮类化合物的构效关系进行分析总结,为后期该类新型抗菌化合物的设计合成提供参考。关键词二氢吲哚-2,3-二酮抑菌活性ResearchProgressinAntibacterialActivityofIndoline-2,3-dioneDerivativesTanHuayuan1,ZhangGuanglong1,JiLitao1,WangQin1,LuYiduo1,OuyangGuiping1,WangZhenchao1,2,3*,LiZhurui1,2*(1SchoolofPharmaceuticalScience,2StateKeyLaboratoryBreedingBaseofGreenPesticideandAgriculturalBioengineering/KeyLaboratoryofMinistryofEducation,GuizhouUniversity;3GuizhouEngineeringLaboratoryforSyntheticDrugs,Guiyang,550025)AbstractIndoline-2,3-dioneisasmalldrugmoleculewithsimplestructureandwideapplication.Thesyntheses,structuresandpharmacologicalactivitiesofitsderivativeshaveattractedmuchattention.Ithasbeenreportedthatindoline-2,3-dionehasvariousbiologicalactivitiessuchasantibacterial,antiaging,hypolipidemic,antiepilepticandantiviralactivities.Thispapermainlyfocusesontheantibacterialbiologicalactivity,andanalyzesandsummarizesthestudiesonstructure-activityrelationshipofindoline-2,3-dionecompoundsathomeandabroad,andprovidesareferenceforthedesignandsynthesesofsuchnewantibacterialcompoundsinfutrue.KeywordsIndoline-2,3-dione,Antibacterialactivity耐药细菌的出现及在全球范围内的传播已经对人类生命和生活环境构成了严重威胁,迫切需要开发新型高效的抗菌候选药物。二氢吲哚-2,3-二酮又名靛红...