丹皮酚吗啉杂合物的合成及抗血小板聚集活性  

Synthesis and Anti-Platelet Aggregation Activity of Paeonol-Morpholine Hybrids

作　　者：顾宏霞[1] 戴卫国 尚飞扬 何黎琴 Gu Hongxiao;Dai Weiguo;Shang Feiyang;He Liqin(West Anhui Health Vocational College,Liuan,Anhui 237000,China;College of Pharmacy,Anhui University of Chinese Medicine,Hefei,Anhui 230038,China)

机构地区：[1]皖西卫生职业学院,安徽六安237000 [2]安徽中医药大学药学院,安徽合肥230038

出　　处：《化学世界》2023年第1期26-29,共4页Chemical World

基　　金：安徽省教育厅自然科学重点科研(No.KJ2020A0957);安徽省高校青年骨干人才国内访学研修(No.gxgnfx2020147);安徽省省级质量工程(No.2020zyq89)资助项目。

摘　　要：以丹皮酚为起始原料,在碱性条件下丹皮酚的2-位酚羟基与二溴烷烃经Williamson反应得到中间体丹皮酚溴代烷基醚2a~2e,化合物2a~2e与吗啉经N-烷基化反应得到丹皮酚吗啉杂合物3a~3e。目标化合物3a~3e经过核磁共振氢谱(1H NMR)、红外(IR)和高分辨质谱(HRMS)表征。体外抗血小板聚集活性测试结果表明,所得目标化合物3a~3e对二磷酸腺苷(ADP)所诱导的血小板聚集均具有较强的抑制活性,优于阳性对照药阿司匹林。The intermediates of paeonol bromoalkyl ester derivatives 2a~2e were obtained via Williamson reaction by treating paeonol with dibromoalkanes(2~6 carbons). 2a~2e were then converted to paeonol-morpholine hybrids 3a~3e through N-Alkylation by reacting with morpholine. The chemical structure of target compounds 3a~3e was confirmed by ~1H NMR, IR and HRMS. The results of pharmacodynamic tests In vitro showed that all of target compounds 3a~3e can significantly inhibit the platelet aggregation induced by Aggregation inhibition(ADP), and the effect was better than that of aspirin.

关 键 词：丹皮酚 有机胺 抗血小板聚集 

分 类 号：R916[医药卫生—药学]