| 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 |
| 投稿时间：2012-04-24 修订日期：2013-01-06 点此下载全文 |
| 引用本文：钟涵宇,张一凯,张敬一,李科.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[J].药学实践杂志,2014,32(2):102~106 |
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| 基金项目:国家自然科学基金(30973640). |
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| 中文摘要: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。 |
| 中文关键词:3-取代呋喃羧酸类化合物 合成 抗凝血 |
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| Synthesis and anti-platelet aggregative activity of novel 2, 5-dihydrofuran derivatives |
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| Abstract:Objective To study the synthesis and anti-platelet aggregative activity of 2-(4-methoxyphenyl)-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives.Methods 17 target compounds were designed, synthesized and determined via 1H-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. Conclusion 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. |
| keywords:pyridazinones synthesis antiplatelet aggregation activity |
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