有机化学 ›› 2008, Vol. 28 ›› Issue (09): 1578-1583. 上一篇    下一篇

研究论文

川芎嗪芳酸衍生物的合成及抗血小板聚集活性

李家明*,a ; 赵永海a ; 马逢时a ; 汪志勇b ;何 勇a ; 张德帅a ; 任海波a
  

  1. (a安徽中医学院药学院 安徽省现代中药重点实验室 合肥 230031)
    (b中国科学技术大学化学系 合肥 230026)
  • 收稿日期:2008-01-18 修回日期:2008-03-27 发布日期:2008-09-20
  • 通讯作者: 李家明

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

LI, Jia-Ming*,a ; ZHAO, Yong-Haia; MA, Feng-Shia; WANG, Zhi-Yongb
HE, Yonga ; ZHANG, De-Shuaia; REN, Hai-Boa
  

  1. (a Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy,
    Anhui College of Traditional Chinese Medicine, Hefei 230031)
    (b Department of Chemistry, University of Science and Technology of China, Hefei 230026)
  • Received:2008-01-18 Revised:2008-03-27 Published:2008-09-20
  • Contact: LI, Jia-Ming

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, 1H NMR, 13C NMR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.

关键词: 川芎嗪, 抗血小板聚集, 阿魏酸, 血栓, 川芎嗪芳酸衍生物

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 1a was 5.7 times than ozagrel.

Key words: ligustrazine, ligustrazine-aromatic acid derivative, platelet aggregation inhibitory, thrombosis, ferulic acid