哒嗪酮类新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

目的研究引入取代仲胺类基团对6-(4-取代乙酰氨基苯基)-5-甲基-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1H-NMR谱等确证;参考文献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9c,9f和9j的抗血小板凝集活性明显优于对照药MCI-154和CCI-17910。结论取代仲胺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-substitued acetamino-phenyl 4, 5-dihydro-3 （2H）-pyridazinones with different substituted secondary amines. Methods Ten target compounds were designed and synthesized. All of them were confirmed by ^1 H-NMR spectra. Born method was applied for prehminary 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 antiplatclet aggregative activity to a certain extent. Compounds 9c, 9f and 9j were better than MCI-154 and CCI-17910 in vitro. Conelution The steric hindrance and hydrophilicity of different substituted secondary amines impact the anti-platelete aggative activity.