川芎嗪芳酸衍生物的合成及抗血小板聚集活性  

Synthesis of Ligustrazine-Aromatic Acid Derivatives and Their Inhibitory Effect on Platelet Aggregation

作　　者：李家明[1] 赵永海[1] 马逢时[1] 汪志勇[2] 何勇[1] 张德帅[1] 任海波[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,合肥230031 [2]中国科学技术大学化学系,合肥230026

出　　处：《有机化学》2008年第9期1578-1583,共6页Chinese Journal of Organic Chemistry

基　　金：安徽省自然科学基金(No.070413118)资助项目

摘　　要：以具有活血化淤作用的中药有效成分川芎嗪、阿魏酸为先导物,按药物化学拼合原理,设计合成了6个全新结构的川芎嗪芳酸衍生物,其结构经IR,1HNMR,13CNMR及MS确证.体外药效筛选结果显示,部分川芎嗪芳酸衍生物对二磷酸腺苷(ADP)诱导的血小板聚集具有较好的抑制活性,其中川芎嗪阿魏酸拼合物(1a)的抑制活性是奥扎格雷的5.7倍.Ligustrazine and ferulic acid, which are useful compounds of Chinese traditional medicine, were used as leading compounds. Six ligustrazine-aromatic acid derivatives were designed and synthesized based on the twin drug principle. Their structures were characterized by IR, ^1H NMR, ^13C NMR and mass spectra. In the in vivo experiment, some compounds have significant inhibitory effect on adenosine diphosphate （ADP） induced platelet aggregation. Among them, the inhibitory effect of compound la was 5.7 times than ozagrel.

关 键 词：川芎嗪 阿魏酸 川芎嗪芳酸衍生物 血栓 抗血小板聚集 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]