6-(4-取代乙酰氨基苯基)-4，5-二氢-3(2H)哒嗪酮衍生物的合成及其抑制血小板聚集活性

Synthesis and the antiplatelet aggregative activity of 6-(4-substituted acetamidophenyl)-4,5-dihydro-3(2H)-pyridazinones

目的：研究引入杂环类基团对6-（4-取代乙酰氨基苯基）_4，5-二氢-3（2H）哒嗪酮类化合物抗血小板凝集活性的影响。方法：设计合成未见报道的目标化合物10个，所有化合物均经过。H—NMR谱等确证；参考Born方法进行体外药理实验。结果：所有化合物都具有抗血小板凝集的活性，其中化合物（5），（9）和（10）的抗血小板凝集活性明显优于MCI-154。结论：杂环基团的空间位阻和亲水性对化合物抗血小板凝集的活性有影响。

Objective ：To study the antiplatelet aggregative activity of 6-（4-substituted acetamido-phenyl） -4,5-dihydro-3 （2H） -pyridazinones with different heterocylic groups. Methods： Ten target compounds were designed and synthesized. All of them were confirmed by ^1H-NMR spectra. Born method was applied for preliminary pharmacological test in vitro. Results：All of the target compounds were reported. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent. Compound （5） , （9） and （10） were better than MCI-154 in vitro. Conclusion： The stereospecific blockade and hydrophilicity of different heterocylic groups impacted the antiplatelet aggregative activity.