Synthesis of Novel Aminothiazolyl Tetrahydroprotoberberrubines with Multi-targeting Antimicrobial Potentiality
作者单位：Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University
会议名称：《中国化学会第十四届全国有机合成化学学术研讨会》
会议日期：2017年
学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学]
基 金：supported by the National Natural Science Foundation of China(no.21672173,21372186) Chongqing Special Foundation for Postdoctoral Research Proposal(no.Xm2016039) State Administration of Foreign Experts Affairs(SAFEA):Introduction of Overseas Young Talents P.R.China(no.WQ2017XNDX047) the Fundamental Research Funds for the Central Universities(no.XDJK2016E059
关 键 词：Aminothiazole Antibacterial Acinetobacter baumanii THPB
摘 要：Berberine is a natural isoquinoline quaternary alkaloid from many kinds of naturally medicinal *** has paid extensive attention as a validated antibacterial agent in China for more than 2000 ***(THPB)as one of the berberine derivatives can improve the molecular flexibility to a certain extent,which may be conducive to enhancing the water solubility and bioavailability,and is a valid structural alternative with widely medicinal *** moiety is present in a variety of clinical drugs and the successful development of many clinical aminothiazole-based drugs has been motivating more and more efforts to develop new bioactive molecules on the basis of this ***,a series of 2-aminothiazolyl THPBs as novel antibacterial agents were designed and *** preliminary research revealed that hexyloxyl THPB derivative 9c should be a new promising multi-targeting candidate with intercalating DNA and/or damaging the cell membrane towards drug-resistant Gram-negative Acinetobacter baumanii.