阿魏酸酯类衍生物的合成及抗血小板聚集活性
Synthesis and anti-platelet aggregation activities of ferulic acid esters
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摘要: 目的 ： 研究阿魏酸酯类衍生物的合成及其抗血小板聚集活性，为研制新型抗血栓药物奠定基础。 方法 ： 采用前药设计原理，将阿魏酸与醇反应形成单酯，再通过拼合原理，将阿魏酸单酯与阿司匹林反应形成双酯；通过体外抗血小板聚集试验对目标化合物进行抗血小板聚集活性评价。 结果 ： 合成了16个目标化合物和8个副产物，其中新化合物15个，其结构经IR、MS和1H NMR确证。活性评价结果表明，部分化合物在体外显示出较好的抗血小板聚集活性。 结论 ： 碳链碳数为4～5的阿魏酸单酯与阿司匹林合成的双酯抗血小板聚集活性较好，可作为先导物进一步研究。Abstract: Aim ：To study the synthesis and anti-platelet aggregation activities of ferulic acidic esters so as to search for novel antithrombus agents. Methods ：Based on prodrug strategy and combination principles，monoesters were first synthesized by reaction of ferulic acid with alcohols，and then the monoesters were coupled with aspirin to afford bis-esters.The target compounds were assayed for anti-platelet aggregation activities in vitro. Results ：Sixteen target compounds and eight sideproducts including 15 new compounds were synthesized and their structures were determined by IR，MS and 1H NMR.The results demonstrated that some tested compounds exhibited potential anti-platelet aggregation activities. Conclusion ：The bis-esters of ferulic esters coupling with aspirin with 4 to 5 carbons in side chain might be used as lead compounds for further study in searching for novel antithrombus agents.
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Keywords:
- ferulic acid /
- esterification /
- aspirin /
- prodrug theory /
- combination principles /
- anti-platelet aggregation
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