7-二乙氨基香豆素腙及酰腙衍生物的制备及乙酰胆碱酯酶抑制活性研究  

Syntheses and Acetylcholinesterase Inhibitory Activities of 7-Diethylaminocoumarin-Based Hydrazone/Acylhydrazone Derivatives

作　　者：於祥 陈娅芳 赵友芳 黄国娟 Yu Xiang;Chen Yafang;Zhao Youfang;Huang Guojuan(College of Pharmacy,Guizhou University of Traditional Chinese Medicne,Guiyang,550025)

机构地区：[1]贵州中医药大学药学院

出　　处：《化学通报》2020年第1期92-95,共4页Chemistry

基　　金：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);大学生创新创业项目([2017]158)资助

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. 32μmol/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。Thirteen 7-N,N-diethylaminocoumarin-based hydrazone/acylhydrazone derivatives were synthesized from 7-N,N-diethylamino-4-methylcoumarin via oxidation with Se O2,and then reacting with substituted hydrazine and acylhydrazine by using the impregnation method.Their structures were confirmed by melting point,1 H NMR and MS.Preliminary bioassay results showed that compounds 4 a and 4 c had potential inhibitory activity against acetylcholinesterase,and their IC50 values were 42.89 and 90.32μmol/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.

关 键 词：香豆素 乙酰胆碱酯酶抑制剂 衍生物 合成 

分 类 号：TQ463[化学工程—制药化工]