NO供体型烟酸衍生物的合成及其生物活性研究  

Synthesis and Biological Evaluation of Nitric Oxide Releasing Nicotinic Acid Derivatives

作　　者：汪电雷[1] 吴亚先[1] 陈维珍[1] 何黎琴[1] 王效山[1] 

机构地区：[1]安徽中医学院药学院安徽省现代中药重点实验室,安徽合肥230031

出　　处：《化学世界》2013年第3期165-168,共4页Chemical World

基　　金：安徽省教育厅自然科学重点研究项目(20120903107)

摘　　要：为寻找活性更强、副作用更小的烟酸前体药物,以烟酸为先导物,设计、合成了5个硝酸酯类NO供体型烟酸衍生物。经红外光谱、核磁共振氢谱及质谱确证了该目标化合物的化学结构。通过体外抗血小板聚集试验、及体内调血脂作用对目标化合物进行生物活性评价。结果表明目标化合物具有较强的体外抗血小板聚集活性及体内良好的降脂作用。To screen out nicotinic acid prodrugs with better activity and less side effects,five nicotinic acid derivatives conjugated with nitric oxide（NO） donor were designed and synthesized from nicotinic acid as leading compound.Their structures were characterized by IR,MS and 1H NMR spectroscopy.Anti-platelet aggregation and lipidemic-modulating activities of the target compounds were evaluated.It was found that all of the synthesized compounds possessed good anti-platelet aggregation and lipidemic-modulating action.

关 键 词：烟酸 硝酸酯 NO供体 抗血小板聚集 调脂作用 

分 类 号：R284[医药卫生—中药学]