Synthesis of Potential MRSA DNA-targeting Naphthalimide Aminothiazoles as Novel Antimicrobial Agent
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 National Natural Science Foundation of China [(No.21372186,21672173) the Research Fund for International Young Scientists from International(Regional)Cooperation and Exchange Program(No.81650110529)]
关 键 词：naphthalimide aminothiazole Hantsch thiazole synthesis antibacterial MRSA
摘 要：A series of novel naphthalimide aminothiazoles were synthesized for the first time via multi-step reactions starting from commercial 4-bromo-1,8-naphthalic *** derivatives 2a-c were accomplished successfully by the typical Hantsch thiazole synthetic *** of the C–Br bond was achieved using alicyclic amines without any *** evaluation revealed that compound 3d could inhibit the growth of MRSA at low concentration（MIC=4μg/m L）,4-fold more potent than *** 3d could also effectively intercalate into MRSA DNA to form 3d–DNA complex,which might be responsible for the powerful bioactivity.