摘要
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.
出处
《药学实践杂志》
CAS
2008年第4期278-281,共4页
Journal of Pharmaceutical Practice
基金
上海市长宁区科委资助课题(20054Y17001)