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

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。

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

Thirteen 7-diethylaminocoumarin-based hydrazone/acylhydrazone derivatives were synthesized from 7-diethylamino-4-methylcoumarin via oxidation with SeO2, and then reacting with substituted hydrazine and hydrazideby using the impregnation method. Their structures were confirmed by melting point, 1H NMR and MS. Preliminary bioassay result of these derivatives" activities inhibiting acetylcholinesterase in vivo showed that compounds 4a and 4c had potential inhibitory activities with 72.1% and 43.1%, respectively. The preliminary structure-activity relationships indicated that acyldrazone derivatives had more inhibitory activities than hydrazone derivatives.