丹皮酚腙类化合物的合成及其抗菌活性  

Synthesis and antimicrobial activity of paeonol derivatives containing hydrazone moiety

作　　者：庞富华 龚红菲[1] 王秀[1] 李芳耀[1] 黄琳[1] 林家迅 

机构地区：[1]桂林医学院药学院,广西桂林541004

出　　处：《化学研究与应用》2018年第1期164-168,共5页Chemical Research and Application

基　　金：广西自然科学基金项目(2015GXNSFAA139035)资助;广西教育厅科研项目(YB2014278)资助;广西脑与认知神经科学重点实验室开放课题项目资助;国家级大学生创新创业训练计划项目(281518681884)资助

摘　　要：根据拼接原理将活性基团腙引入中药活性成分丹皮酚中对其结构进行修饰,以丹皮酚为原料,与80%水合肼在乙醇中反应得到中间体丹皮酚腙(2),然后与芳香醛反应合成了10个芳甲叉基丹皮酚腙(3a-3j),其结构经IR、~1H NMR、^(13)C NMR和ESI-MS表征。采用二倍稀释法测定目标化合物对金黄色葡萄球菌和大肠杆菌的最低抑菌浓度(MIC),结果表明:大部分化合物金黄色葡萄球菌和大肠杆菌表现出较好的抑菌活性,特别是化合物3i对金黄色葡萄球菌的的MIC为2μg·mL^(-1),优于阳性对照药环丙沙星。Paeonol was modified by active functional group hydrazone according to the combination principle. The intermediate hydrazone（2） was synthesized by condensation reaction of paeonol with 80% hydrazine hydrate in 95% ethanol. Ten novel paeonol hydrazine compounds （ 3a-3j ） were prepared by the reaction of 2 and appropriate arylaldehydes. T h e ir structures were characterized by IR,^1H NMR,^13C NMR,and ESI-MS. The minimal inhibitory concentrations （M/C） of target compounds against S. aureus and E. coli. were determined by two times dilution method. The results showed that most of the tested compounds displayed good antimicro-bial activities. In particular,compound 3i exhibited better in h ibito ry activities than ciprofloxacin against S. aureus.

关 键 词：丹皮酚 腙 抗菌活性 合成 

分 类 号：O621.3[理学—有机化学]