新型哒嗪酮衍生物的合成及其对血小板聚集的抑制作用

Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

目的合成新的含有胺基的哒嗪酮类化合物,并研究其对此类化合物抗血小板聚集活性的影响。方法设计合成未见报道的目标化合物9个,所有化合物均经过H-NMR谱等确证;参考文献方法进行体外药理实验。结果发现所有化合物都具有抗血小板凝集的活性,其中化合物9c,9e和9i的抗血小板凝集活性明显优于对照化合物MCI-154和CCI-17910。结论引入不同的取代胺基,对化合物抑制血小板聚集的活性有影响。

Objective To study the antiplatelet aggregative activity of 6-（4-substitued acetamino-phenyl 4,5-dihydro-3（2H）- pyridazinones with different amino group. Methods Nine target compounds were designed and synthesized. All of them were confirmed by 1 H-NMR spectra. Born method was applied for preliminary pharmacological test in vitro. Results All of the target compounds were not reported. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggrega- rive activity to a certain extent. Compounds 9c, 9e and 9i were better than MCI-154 and CCI-17910 in vitro. Conclusion Inletting dif- ferent substituted amino groups could enhance the antiplatelet aggregation activity of the compounds.