4,5-二氢-3(2H)-哒嗪酮类化合物的合成及其对血小板聚集的抑制作用

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

目的:合成新的哒嗪酮类化合物,并研究其抗血小板凝集活性。方法:在6-(4-氯乙酰氨基苯基)-4,5-二氢-3(2H)哒嗪酮引入不同取代哌嗪,合成一系列化合物,并经过1H-NMR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(1)、(4)的抗血小板凝集活性明显优于MCI-154。结论:4-位取代哌嗪环基的引入对化合物抗血小板凝集的活性有显著影响。

Objective ： To study the antiplatelet aggregative activity of 6- （ 4-substituted acetamido-phenyl ） -4,5-dihydro-3 （2H） -pyridazinones inletting different piperazine groups. Methods： Ten 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 reported. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent. Compound（ 1 ）/（4 ）and performed better than MCI-154 in vitro. Conclusion：The carbochain＇s length of piperazine＇s 4-substituted groups impacted the antiplatelet aggregative activity promintly.