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.
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)
出处
《化学通报》
CAS
CSCD
北大核心
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
关键词
香豆素
乙酰胆碱酯酶抑制剂
衍生物
合成
Coumarin
Acetylcholinesterase inhibitor
Derivatives
Synthesis