丹皮酚哌嗪衍生物的设计与体外抗血小板聚集研究

Research on Design of Paeonol Piperazine Derivatives and Extracorporal Antiplatelet Aggregation

以丹皮酚为模型化合物,依据生物电子等排原理,设计了3个丹皮酚哌嗪衍生物,通过溴代反应、取代反应对其进行了合成,3个丹皮酚衍生物的结构均经MS、1H NMR和13C NMR确证。采用Bron比浊法对其AA、ADP诱导的血小板聚集抑制活性进行了研究。化合物4b对AA、ADP诱导的血小板聚集的抑制活性均优于阳性对照组阿司匹林。

Taking paeonol as model compound,three paeonol piperazine derivatives were designed on grounds of bioisosterism.They are synthesized by bromination reaction and substitution reaction.The structures of three paeonol piperazine derivatives were identified by MS,1H-NMR and 13C-NMR.The inhibitory activity of platelet aggregation,which is induced by AA and ADP,is studied by means of Bron turbidimetry.As to the compound 4b,its inhibitory activity against platelet aggregation,which is induced by AA and ADP,is better than aspirin in control group.