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

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.