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目的为寻找新的更高活性的抗血小板聚集药物,设计制得10个具有4-甲氧基-1,3-苯二磺酸酯结构的目标化合物(系列2);并对其进行体外活性筛选,评价其抗血小板聚集活性并推测其构效关系。方法按照前期工作获得的吡考他胺衍生物构效关系原则,进行了目标物设计合成,其结构均经~1H-NMR、IR和MS谱确证。采用Born比浊法对目标化合物进行了体外抗血小板聚集活性初筛。结果与结论合成的目标化合物均未见文献报道,其中PS27的活性最高,超过两个阳性对照药物吡考他胺和阿司匹林;PS22、PS23、PS24和PS26等4个化合物的活性优于或与对照药物相当。与磺酰胺类化合物相比,磺酸酯类中具有活性的化合物比例更高,在抗血小板聚集方面具有研究价值。
OBJECTIVE To search for new and more active anti-platelet aggregation drugs, 10 target compounds with 4-methoxy-1,3-benzenedisulfonate structure (Series 2) were designed and prepared, and their in vitro activities Screening, evaluation of its anti-platelet aggregation activity and speculated that the structure-activity relationship. Methods According to the principle of structure-activity relationship of the derivatives of picratadine obtained in the previous work, the target compounds were designed and synthesized. Their structures were confirmed by ~ 1H-NMR, IR and MS spectra. The target compounds were preliminarily tested for anti-platelet aggregation activity by Born turbidimetry. RESULTS AND CONCLUSIONS None of the target compounds synthesized were reported in the literature. The activity of PS27 was the highest, exceeding the two positive control drugs, picratamine and aspirin. The activity of four compounds such as PS22, PS23, PS24 and PS26 was better than that of control Drug equivalent. Compared with the sulfonamides, sulfonate compounds with a higher proportion of active in the anti-platelet aggregation has research value.