中文关键词:香豆素乙酰胆碱酯酶抑制剂衍生物合成 英文关键词:CoumarinAcetylcholinesterase inhibitorDerivativesSynthesis 基金项目:贵州中医药大学2018年度学术新苗培养及创新探索专项（黔科合平台人才[2017]5735号-22）、贵州省教育厅青年人才成长项目（黔教合KY字[2017]169）和大学生创新创业项目（[2017]158）资助

作者	单位
於祥	贵州中医药大学药学院 贵阳 550025
陈娅芳	贵州中医药大学药学院 贵阳 550025
赵友芳	贵州中医药大学药学院 贵阳 550025
黄国娟	贵州中医药大学药学院 贵阳 550025

摘要点击次数:772 全文下载次数:0 中文摘要: 本论文采用亚活性结构拼接的方法，以7-N，N-二乙氨基-4-甲基香豆素为原料，经二氧化硒氧化，然后与取代肼和取代酰肼反应，合成了13个7-N，N-二乙氨基香豆素腙及酰腙衍生物。所有目标化合物经¹H NMR和MS进行结构确证。体外抑制乙酰胆碱酯酶活性结果表明，目标化合物4a和4c对乙酰胆碱酯酶具有较强的抑制活性，其IC₅₀值分别为42.89和90.32 μmol/L。初步构效关系研究表明，酰腙衍生物对乙酰胆碱酯酶的抑制活性比腙类衍生物好。 英文摘要: Thirteen 7-N,N-diethylaminocoumarin-based hydrazone/acylhydrazone derivatives were synthesized from 7-N,N-diethylamino-4-methylcoumarin via oxidation with SeO₂, and then reacting with substituted hydrazine and acylhydrazine by using the impregnation method. Their structures were confirmed by melting point, ¹H NMR and MS. Preliminary bioassay results showed that compounds 4a and 4c had potential inhibitory activity against acetylcholinesterase, and their IC₅₀ values were 42.89 and 90.32 μmol/L, respectively. The preliminary study on the structure-activity relationships indicated that acylhydrazone derivatives have better inhibitory activity against acetylcholinesterase than those of the hydrazone derivatives. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书 -->