吡考他胺类似物的合成及其抑制血小板聚集作用

Synthesis and platelet aggregation inhibitory activities of the analogs of picotamide

目的为寻找新的抗血小板聚集剂,以抗血小板聚集药物吡考他胺(picotamide)为先导化合物,对其结构进行改造,合成新的类似物。方法以苯甲醚为原料,经3步反应制得中间体4-甲氧基-1,3-苯二甲酰氯,经与不同的胺类化合物进行取代反应制得目标化合物。结果与结论共制得10个新化合物,其结构经红外和核磁共振谱确证。药理实验结果表明,化合物PN9和PN10的抗血小板聚集活性很高,明显优于阳性对照药物picotamide。

Aim To search new antiplatelet aggregating agents, a series of novel compounds were synthesized through taking picotamide as lead compound. Method With 4-methoxy-1, 3-benzenedicarboxyl chloride and different arylamides as starting material, ten target compounds were synthesized. Results and conclusion The structures of ten novel compounds were confirmed by IR and ^1H-NMR spectroscopy and the activities in vitro of the compounds on antiplatelet aggregation were tested and assessed. Compounds PN9 and PN10 have significant antiplatelet aggregation activity, superior to that of the reference drug picotamide.