丹皮酚席夫碱衍生物的合成及其生物活性研究  

Synthesis and Biological Evaluation of Paeonol-Nitrate Derivatives

作　　者：纪孟姣 柏志伟 王宇 何黎琴 Ji Mengjiao;Bai Zhiwei;Wang Yu;He Liqin(College of Pharmacy,Anhui University of Chinese Medicine,Hefei,Anhui 230038,China)

机构地区：[1]安徽中医药大学药学院,安徽合肥230038

出　　处：《化学世界》2020年第7期487-490,共4页Chemical World

基　　金：安徽省教育厅自然科学重点科研(No.KJ2017A292);国家级2017年大学生创新创业训练计划(No.2017045)资助项目。

摘　　要：以丹皮酚与甘氨酸为原料制备含席夫碱结构的丹皮酚中间体,利用其羧基与不同碳数的二溴烷烃反应得到相应的丹皮酚亚胺基乙酸溴代烷基酯衍生物3a^3e,再与硝酸银反应生成丹皮酚硝酸酯衍生物4a^4e。化合物4a^4e的结构经过红外光谱、核磁共振氢谱和质谱表证。对合成的丹皮酚硝酸酯类衍生物进行体外抗血小板聚集及体内调血脂作用的生物活性测试,结果表明,化合物4a^4e均具有一定的体外抗血小板聚集活性及较强的体内降脂作用。Paeonol amino-acid schiff base was synthesized by the reaction of paeonol(1)with glycine so that it could react with dibromoalkanes bearing two to six carbons to form the compounds 3 a^3 e.These compounds were then treated with silver nitrate to yield paeonol-nitrate derivatives 4 a^4 e.Five target compounds were characterized by IR,MS,and^1H NMR.Anti-platelet aggregation and lipidemic-modulating activities of target compounds were evaluated.It was found that all of synthesized compounds possessed anti-platelet aggregation and stronger lipidemic-modulating action.

关 键 词：丹皮酚 席夫碱 抗血小板凝集 调脂作用 

分 类 号：R916[医药卫生—药学]