川芎嗪芳酸醚甘氨酸衍生物合成及抗血小板聚集活性  

Synthesis of a series of glycine derivatives ligustrazine-aromatic acid and their inhibitory effects on platelet aggregation

作　　者：邬皓[1] 李家明[1] 盛日正[1] 周鹏[1] 钟国琛[1] 蒋丽娜[2] 

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,合肥230031 [2]安徽大学,安徽合肥230601

出　　处：《安徽医药》2011年第8期937-940,共4页Anhui Medical and Pharmaceutical Journal

基　　金：国家科技重大专项重大新药创制项目(批准号:2009ZX09103-123);安徽省高校自然基金重点项目(批准号:KJ2010A206)

摘　　要：目的合成一系列新的甘氨酸衍生物,并初步筛选其抗血小板聚集活性。方法以川芎嗪、甘氨酸、阿魏酸等芳酸为起始原料,经过一系列反应,合成得到目标化合物。结果合成了6个川芎嗪芳酸醚类甘氨酸衍生物,其结构均经IR、1H-NMR、13C-NMR和MS确证。结论所有目标化合物均未见文献报道。药理结果初步显示化合物1a、1b、1c、1d、1e、1f血小板抑制率分别为8.2%、6.5%、15.9%、6.7%、5.1%、3.2%。Aim To synthesize a series of new glycine derivatives and to study their inhibitory effects on platelet aggregation.Methods The target compounds were synthesized from Ligustrazine,glycine,ferulic acid and its analogs via a series of reactions.Results Six target compounds were synthesized.Their structures were characterized by IR,1H-NMR,13C-NMR and MS.Conclusions The target compounds have not been reported in literatures.Preliminary pharmacological results show that the inhibitory effect on platelet aggregation of compounds 1a,1b,1c,1d,1e,1f is 8.2%,6.5%,15.9%,6.7%,5.1%,and 3.2%.

关 键 词：川芎嗪 甘氨酸 抗血小板聚集 化学合成 

分 类 号：R284.3[医药卫生—中药学]