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目的寻找新的高效低毒的血小板聚集抑制剂。方法 4-甲氧基-N,N’-二苯基-1,3-苯二甲酰胺为先导化合物,用4-取代苯氧基代替苯氨基对先导化合物进行结构改造:以苯甲醚为原料,采用文献方法经3步反应制得重要中间体4-甲氧基-13,-苯二甲酰氯;该中间体与4-取代苯酚类化合物进行取代反应制得目标化合物。以吡考他胺和阿司匹林为阳性对照药物,采用Born比浊法对目标化合物进行体外抗血小板聚集活性初筛。结果与结论包括先导化合物在内共制得9个化合物,其中8个未见文献报道。目标化合物的化学结构均经IR1、H-NMR和MS谱确证。药理试验结果表明,化合物PO3的抗血小板聚集活性最高,优于吡考他胺和阿司匹林,化合物PO4、PO5和PO7的活性超过吡考他胺。
Objective To find a new inhibitor of platelet aggregation with high efficiency and low toxicity. Methods 4-Methoxy-N, N’-diphenyl-1,3-benzenedicarboxamide was used as the lead compound to replace the anilino group with 4-substituted phenoxy group. Raw materials, the literature method using 3 steps to obtain the important intermediate 4-methoxy-13, - phthaloyl chloride; This intermediate and 4-substituted phenolic compounds for substitution reaction of the target compound. Pirratamine and aspirin as positive control drugs, the Born turbidimetric method for the target compound for anti-platelet aggregation activity in vitro screening. RESULTS AND CONCLUSIONS Nine compounds including lead compounds were prepared, of which eight were not reported in the literature. The chemical structures of the target compounds were confirmed by IR1, H-NMR and MS spectra. Pharmacological test results show that compound PO3 has the highest anti-platelet aggregation activity superior to picotamide and aspirin, and the compounds PO4, PO5 and PO7 are more active than picotamide.