| 尚飞扬,丁乐,何黎琴,顾宏霞,徐路安.化学通报,2022,85(4):480-484. |
| 7-羟基-3-乙酰基香豆素曼尼希碱衍生物的合成及抗血小板聚集活性 |
| Synthesis and Anti-platelet Aggregation Activity of 7-hydroxy -3- acetyl Coumarin Mannich base Derivatives |
| 投稿时间：2021-07-09 修订日期：2021-09-16 |
| DOI： |
| 中文关键词: 7-羟基-3-乙酰基香豆素 曼尼希碱 肟 抗血小板聚集 |
| 英文关键词:7-hydroxy-3-acetyl-coumarin Mannich base oxime anti-platelet aggregation |
| 基金项目: |
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| 中文摘要: |
| 以间苯二酚为起始原料，经Vilsmeier-Haack反应、Knoevenagel反应及Mannich反应得到中间体7-羟基-3-乙酰基香豆素曼尼希碱，再将其酮羰基肟化得到目标化合物。采用Born比浊法，以二磷酸腺苷（ADP）和花生四烯酸（AA）为诱导剂，阿司匹林为阳性对照，对5个目标化合物进行了的体外抗血小板聚集的活性试验，结果表明，目标化合物对ADP和AA诱导的血小板聚集均具有较强的抑制作用，且大部分明显优于阿司匹林。 |
| 英文摘要: |
| Starting from ?resorcinol，intermediates 3 (7-hydroxy-3-acetyl-coumarin Mannich base) were obtained through Vilsmeier-Haack, Knoevenagel reaction and Mannich reaction, which was then treated with NH2OH to give the target compounds 7-hydroxy-3-acetyl-coumarin Mannich base oximes derivatives(5a~5e). The chemical structure of target compounds was confirmed by 1H NMR, IR and HRMS. The anti-platelet aggregation activity of 5a~5e was tested by Born turbidimetry using ADP and AA as inducers. The results of pharmacodynamic tests showed that the platelet aggregation induced by ADP and AA induced were significantly inhibited and the effect was better than that of aspirin. |
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