| 7-硝氧烷氧基-3-乙酰基香豆素的合成及抗血小板聚集活性 |
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| 引用本文： | 尚飞扬,戴卫国,何冰,何黎琴.7-硝氧烷氧基-3-乙酰基香豆素的合成及抗血小板聚集活性[J].化学世界,2022,63(1):17-21. |
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| 作者姓名： | 尚飞扬 戴卫国 何冰 何黎琴 |
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| 作者单位： | 安徽中医药大学药学院,安徽合肥230038 |
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| 基金项目： | 安徽省教育厅自然科学重点科研(No.KJ2020A0957)资助项目； |
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| 摘 要： | 以间苯二酚为起始原料,经Vilsmeier-Haack反应、Knoevenagel反应得到7-羟基-3-乙酰基香豆素(3),再利用其7位羟基通过连接臂与有机硝酸酯类NO供体耦合,得到5个7-硝氧烷氧基-3-乙酰基香豆素(5a～5e).目标化合物经过红外光谱(IR)、核磁共振氢谱(1H NMR)和高分辨质谱(HRMS)表...
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| 关 键 词： | 7-羟基-3-乙酰基香豆素 硝酸酯 抗血小板聚集 |
Synthesis and Anti-Platelet Aggregation Activity of 7-Nitratoalkoxyl-3-acetyl-coumarin |
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| Shang Feiyang,Dai Weiguo,He Bing,He Liqin.Synthesis and Anti-Platelet Aggregation Activity of 7-Nitratoalkoxyl-3-acetyl-coumarin[J].Chemical World,2022,63(1):17-21. |
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| Authors: | Shang Feiyang Dai Weiguo He Bing He Liqin |
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| Affiliation: | (College of Pharmacy,Anhui University of Chinese Medicine,Hefei,Anhui 230038,China) |
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| Abstract: | 7-Hydroxy-3-acetyl-coumarin was obtained from resorcinol by Vilsmeier-Haack and Knoevenagel reactions, which was then treated with dibromoalkanes(2~6 carbons) in the presence of K;CO;to provide 7-bromoalkoxyl-3-acetyl-coumarin(4 a~4 e). Compounds 4 a~4 e reacted with silver nitrate to give the target compounds of 7-nitratoalkoxyl-3-acetyl-coumarin(5 a~5 e). Their structures were confirmed by IR,;H NMR and high-resolution mass spectrometry(HRMS). The anti-platelet aggregation activity of 5 a~5 e was tested by Born turbidimetry using adenosine diphosphate(ADP) and collagen as inducers. It was found that the synthesized compounds had inhibitory effects on both ADP and collagen-induced platelet aggregations. Compound 5 d exhibited excellent activity than the reference drug aspirin. |
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| Keywords: | 7-hydroxy-3-acetyl-coumarin nitrate anti-platelet aggregation |
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