烃基丹皮酚肟化合物的合成及抗血小板聚集活性  

Synthesis and Anti-Platelet Aggregation Activities of Paeonol Oxime Compounds

作　　者：王蓉[1] 柯江涛 孙恒 毛珝人 何黎琴 Wang Rong;Ke Jiangtao;Sun Heng;Mao Xuren;He Liqin(Bozhou Vocational and Technical College,Bozhou,Anhui 236800,China;College of Pharmacy,Anhui University of Chinese Medicine,Hefei,Anhui 200038,China)

机构地区：[1]亳州职业技术学院,安徽亳州236800 [2]安徽中医药大学药学院,安徽合肥200038

出　　处：《化学世界》2021年第4期236-239,共4页Chemical World

基　　金：安徽省教育厅自然科学重点科研(No.KJ2017A292)资助项目。

摘　　要：为探究丹皮酚2-位羟基不同烃基取代对抗血小板聚集活性的影响,合成了7个不同烃基取代的丹皮酚肟衍生物3a~3g并测试了体外抗血小板聚集活性。以丹皮酚为原料,与不同的溴代烃在碱性条件下反应,得到烃基丹皮酚醚,再将其酮羰基肟化,得到7个烃基丹皮酚肟衍生物。目标化合物3a~3g的结构经过红外光谱、核磁共振氢谱和高分辨质谱确证。体外抗血小板聚集活性结果表明,目标化合物3a~3g的活性均强于对照药阿司匹林,其中化合物3a~3b和3g的抗血小板聚集活性显著,血小板聚集抑制率(AIR)是阿司匹林的2.5~3.0倍。To investigate the effects of different alkyl substitutions of paeonol 2-hydroxyl on platelet aggregation activity,seven paeonol derivatives(3 a~3 g)were synthesized and tested for antiplatelet aggregation activity in vitro.The target compounds(alkyl paeonol oxime)3 a~3 g were obtained via alkylation,oximation from paeonol.Their structures were characterized by 1H NMR,IR and HR-ESIMS.The biological screening results demonstrated that all target compounds exhibited potent anti-platelet aggregation activities.Among all the compounds 3 a,3 b and 3 g(with aggregation inhibition rate(AIR)values of 31.23%,27.65%,26.23%,respectively)showed significant anti-platelet aggregation activities stronger than that of control aspirin(AIR:11.14%).

关 键 词：丹皮酚 肟 抗血小板凝集 

分 类 号：O914.5[理学]