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  

Syntheses and Anti-platelet Aggregation Activities of 7-Hydroxy-3-acetyl Coumarin Mannich Base Derivatives

作　　者：尚飞扬 丁乐 何黎琴 顾宏霞[2] 徐路安 Shang Feiyang;Ding Le;He Liqin;Gu Hongxia;Xu Luan(College of Pharmacy,Anhui University of Chinese Medicine,Hefei,230038;West Anhui Health Vocational College,Liuan,237000)

机构地区：[1]安徽中医药大学药学院,合肥230038 [2]皖西卫生职业学院,六安237000

出　　处：《化学通报》2022年第4期480-484,385,共6页Chemistry

基　　金：安徽省教育厅自然科学重点科研项目(KJ2020A0957)资助。

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,且大部分化合物的活性明显优于阿司匹林。Starting from resorcinol, intermediate 3(7-hydroxy-3-acetyl-coumarin) was obtained through Vilsmeier-Haack, Knoevenagel and Mannich reactions, which was then treated with NH;OH to give the target compounds 7-hydroxy-3-acetyl-coumarin Mannich base oxime derivatives(5 a~5 e). The chemical structure of target compounds was confirmed by;H NMR, IR and HRMS. The anti-platelet aggregation activities of 5a~5e were tested by Born turbidimetry using adenosine diphosphate(ADP) and arachidonic acid(AA) as inducers. The results showed that the target compounds have a strong inhibitory effect on platelet aggregation induced by ADP and AA, and their activities are significantly better than that of aspirin.

关 键 词：7-羟基-3-乙酰基香豆素 曼尼希碱 肟 抗血小板聚集 

分 类 号：TQ460.1[化学工程—制药化工]