新型二氢呋喃类化合物的合成及抑制血小板聚集活性研究

目的 研究2-（4-甲氧基苯基）-4-乙烯基-2,5-二氢呋喃-3-羧酸及其衍生物的合成及抗血小板凝集活性.方法 设计合成未见报道的目标化合物17个,应用1H-NMR、MS对得到的目标化合物进行结构鉴定,采用Born方法对目标化合物进行体外抗凝血活性测试.结果 合成得到2-（4-甲氧基苯基）-4-乙烯基-2,5-二氢呋喃-3-羧酸及其衍生物17个,所有目标化合物均具有优于对照药MCI-154的抗血小板凝集活性.结论 2-（4-甲氧基苯基）-4-乙烯基-2,5-二氢呋喃-3-羧酸及其衍生物具有较好的抗凝血药理活性,其中化合物（3）,（6）和（10）的活性分别是到对照药MCI-154的22.2,12.8和8.6倍,具有很强的开发应用前景.

Synthesis and anti-platelet aggregative activity of novel 2, 5-dihydrofuran derivatives

Objective To study the synthesis and anti-platelet aggregative activity of 2-（4-methoxyphenyl）-4-vinyl-2,5-di- hydrofuran-3-carboxylic acid derivatives. Methods 17 target compounds were designed, synthesized and determined via ~ H-NMR spectra and MS. The anti-platelet aggregative activities of the target compounds in vitro were assessed by Born method. Results The results of preliminary pharmacological test showed that all the target compounds had good anti-platelet aggregative activity in vitro and compounds 3, 6 and 10 were the best candidates, which had 22.2, 12.8 and 8.6 times than positive control, respectively. Conclu- sion 2-（4-methoxyphenyl）-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives had a pharmacological activity of anti-coagulation. The anti-platelet aggregative activities of compounds 3, 6 and 10 could be worth to further research.