新型苄基丹皮酚肟衍生物的合成及抗血小板聚集活性  

Synthesis and Anti-platelet Aggregation Activities of Novel Benzyl Paeonol Oxime Derivatives

作　　者：顾宏霞[1] 王宇 戴卫国 何黎琴 GU Hong-xia;WANG Yu;DAI Wei-guo;HE Li-qin(Department of Pharmacy, West Anhui Health Vocational College, Lu’an 237000, China;College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China)

机构地区：[1]皖西卫生职业学院药学系,安徽六安273000 [2]安徽中医药大学药学院,安徽合肥230038

出　　处：《合成化学》2021年第8期686-690,共5页Chinese Journal of Synthetic Chemistry

基　　金：安徽省教育厅优秀拔尖人才培育资助重点项目(gxgnfx2020147);安徽省教育厅自然科学重点科研项目(KJ2017A292);安徽省省级质量工程项目“药学专业群建设”(20202y989)。

摘　　要：为得到抗血小板聚集活性更好的丹皮酚衍生物,在2-位苄基取代的基础上,以丹皮酚为原料,经苄基化,肟化及醚化合成了5个新型的苄基丹皮酚肟衍生物(4a~4e),其结构经^(1)H NMR,IR和HR-MS(ESI)表征。体外抗血小板聚集活性结果表明:4a~4e(AIR:13.87~21.50%)的活性均强于对照药阿司匹林(AIR:11.14%),其中化合物4c(AIR:20.76%)和4e(AIR:21.50%)的抗血小板聚集活性显著,具备进一步研究的潜力。To search for new antiplatelet agents with higher potency,five benzyl paeonol oxime ethers derivatives were synthesized and tested for antiplatelet aggregation activity in vitro.The target compounds(4a~4e)obtained via benzylation,oximation and etherification from paeonol.Their structures were characterized by ^(1)H NMR,IR and HR-MS(ESI).The biological screening results demonstrated that all target compounds(AIR values of 13.87%~21.50%)exhibited potent anti-platelet aggregation activities,which stronger than that of control Aspirin(AIR:11.14%).Among all the compounds,4c and 4e(AIR values of 20.76%,21.50%,respectively)showed significant anti-platelet aggregation activities,which could be considered a lead compound for further modification.

关 键 词：丹皮酚 肟醚 合成 醚化 抗血小板凝集 阿司匹林 

分 类 号：R914.5[医药卫生—药物化学]