Design,synthesis,andbiologicalevaluationofchrysinderivativesaspotentialFabHinhibitors.pdf
Newseriesofchrysinderivatives(4a-4t)weredesignedandsynthesizedbyintroducingdifferentsubstitutedpiperazinesatC-7position.TheirinhibitoryeffectsonFabHwereevaluatedusingtwoGram-negativebacterialstrains,EscherichiacoliandPseudomonasaeruginosa,andtwoGram-positivebacterialstrains,BacillussubtilisandStaphylococcusaureus.Toourdelight,mostofthesecompoundsexhibitedadramaticincreaseininhibitorypotency,comparedwiththecontrolpositivedrugs.Amongthem,compound4sexhibitedthemostpotentinhibitoryactivitywithIC50valuesof5.78±0.24μminhibitingE.coliFabHandpotentantibacterialactivityagainstS.aureusandE.coliwithMICof1.25±0.01,1.15±0.12μg/mL,respectively,comparingtothecontrolpositivedrugspenicillinG(7.56±0.30μm).Dockingsimulationwasperformedtopositioncompound4sintotheFabHactivesite,andtheresultshowedthatcompound4scouldbindwellwiththeFabHaspotentFabHinhibitor.
作者：Hong-XiaLi Zhong-ChangWang Yu-MeiQian Xiao-QiangYan Ya-DongLu Hai-LiangZhu
作者单位：SchoolofLifeandFoodEngineering,SuzhouUniversity,SuzhouAnhui,People'sRepublicofChina;StateKeyLaboratoryofPharmaceuticalBiotechnology,NanjingUniversity,Nanjing,People'sRepublicofChinaStateKeyLaboratoryofPharmaceuticalBiotechnology,NanjingUniversity,Nanjing,People'sRepublicofChinaSchoolofLifeandFoodEngineering,SuzhouUniversity,SuzhouAnhui,People'sRepublicofChinaNeonatalMedicalCenter,NanjingChildren'sHospitalofNanjingMedicalUniversity,Nanjing,JiangsuProvince,China
母体文献：第九届国际分子模拟与信息技术应用学术会议(ICMS&I2018)论文集
会议名称：第九届国际分子模拟与信息技术应用学术会议(ICMS&I2018)
会议时间：2018年5月1日
会议地点：太原
主办单位：中国化学会,中科院,北京创腾科技有限公司
语种：chi
分类号：
关键词：antibacterialactivities chrysinderivatives docking FabH synthesis
在线出版日期：2019年6月27日
基金项目：
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