Synthesis and anti-platelet aggregation activities of ferulic acid esters
10.3321/j.issn:1000-5048.2009.06.002
- VernacularTitle:阿魏酸酯类衍生物的合成及抗血小板聚集活性
- Author:
Baoquan LI
;
Nianguang LI
;
Feng FENG
;
Yuping TANG
;
Jinao DUAN
- Publication Type:Journal Article
- Keywords:
ferulic acid;
esterification;
aspirin;
prodrug theory;
combination principles;
anti-platelet aggregation
- From:
Journal of China Pharmaceutical University
2009;40(6):486-490
- CountryChina
- Language:Chinese
-
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 struc-tures 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 antithrom-bus agents.