丹皮酚肟衍生物的设计、合成及抗血小板聚集活性  

Design,synthesis and anti-platelet aggregation activity of paeonol oxime derivatives

作　　者：戴卫国 谭鸿舟 顾宏霞[2] 何冰 何黎琴 黄鹏 DAI Weiguo;TAN Hongzhou;GU Hongxia;HE Bing;HE Liqin;HUANG Peng(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;West Anhui Health Vocational College,Liuan 237005,China)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]皖西卫生职业学院,六安237005

出　　处：《中国药科大学学报》2022年第5期535-541,共7页Journal of China Pharmaceutical University

基　　金：安徽省高校自然科学研究资助项目(No.KJ2020A0957)。

摘　　要：以丹皮酚为起始原料,经结构修饰得到25个新的丹皮酚肟类衍生物4a~4y,其结构经过高分辨质谱、核磁共振氢谱确证。所合成的目标化合物对二磷酸腺苷(ADP)和胶原诱导的血小板聚集均具有一定的抑制活性,其中化合物4h、4j对两种诱导剂诱导的血小板聚集优于阳性对照药阿司匹林,且化合物4h具有较好的水溶性和类药性,可作为新的抗血小板活性化合物进一步研究。In order to afford new antiplatelet agents with higher potency,a series of paeonol oxime derivatives(4a-4y)were designed and synthesized from paeonol.Their structures were confirmed by HRMS,1H NMR spectra.The anti-platelet aggregation activity of the target compounds was evaluated.The results revealed that most of them had moderate to good anti-platelet aggregation activity.Among them,compound4hand4jwere the most potent on adenosine diphosphate(ADP)-induced platelet aggregation and collagen-induced platelet aggregation.Furthermore,the target compound4hnot only showed strong antiplatelet aggregation activity,but also exhibited good water-solubility and drug-like properties,which can be used as a new antiplatelet active compound for further research.

关 键 词：丹皮酚肟衍生物 合成 水溶性 抗血小板聚集 

分 类 号：R914.5[医药卫生—药物化学] R965[医药卫生—药学]