【作者】 李悦青； 吴茜茜； 宋其玲； 徐艳； 秦秋燕； 赵伟杰；

【Author】 Yueqing Li;Qianqian Wu;Qilin Song;Yan Xu;Qiuyan Qin;Weijie Zhao;School of Pharmaceutical Science and Technology,Dalian University of Technology;

【机构】 大连理工大学制药科学与技术学院；

【摘要】 血小板在血栓形成过程中起关键作用^[1]。本研究以药用植物中具有抗ADP诱导血小板聚集的柄果花椒酰胺为研究对象,以7种苯甲醛衍生物为原料,经过缩合反应及甲基化等反应制得了柄果花椒酰胺及类似物2a²h,3a³h,4a⁴h。对这些化合物进行体外抗血小板聚集活性测试^[2],结果显示:9个类似物的活性均强于柄果花椒酰胺。总结该类化合物的构效关系:4位甲氧基取代对化合物的活性最为有利;甲基化B环中的羟基和结构中的酰胺氮原子可增强化合物活性。更多还原

【Abstract】 Based on seven kinds of benzaldehyde derivatives,a series of podocarpamide analogues were synthesized via condensation reaction and methylation reaction.In vitro antithrombotic activity of these analogues was evaluated.The result showed that nine analogues possessed better platelet aggregation inhibition than podocarpamide.The structure-activity relationship was deduced.4-Methoxy substituent was the most favorable group.Moreover,methylation of hydroxyl group on ring B and the nitrogen atom of amide in the structure can increase antiplatelet aggregation activity.更多还原