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抗血小板凝集活性  

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

作　　者：蔡灵芝[1] 徐建明[1] 胡宏岗[1] 宋琰[1] 孙亮[1] 俞世冲[1] 吴秋业[1] 

机构地区：[1]第二军医大学药学院有机化学教研室,上海200433

出　　处：《中国药物化学杂志》2007年第4期209-212,220,共5页Chinese Journal of Medicinal Chemistry

基　　金：上海市长宁区科研项目(20054Y17001)

摘　　要：目的研究引入仲胺类基团对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13个,用1H-NMR、IR、MS确证结构,参考Born方法进行体外药理实验。结果与结论所有化合物都具有抗血小板凝集的活性,其中化合物6b、6g的抗血小板凝集活性明显优于MCI-154。仲胺类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。Aim To study the antiplatelet aggregative activity of 6-（4-substituted acetamido-phenyl）-4, 5-di- hydro-3 （2H）-pyridazinones inletting different secondary amino groups. Methods Thirteen target compounds were designed and synthesized. All of them were confirmed by ^1H-NMR and parts of them were confirmed by IR, MS spectra. Born method was applied for preliminary pharmacological test in vitro. Results and conclusion All of the target compounds were reported firstly. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent. The activity of compounds 6b and 6g were better than that of MCI-154 in vitro. The stereospecific blockade and hydrophilicity of different secondary amino groups impact the antiplatelet aggregative activity.

关 键 词：化学合成 哒嗪酮类 体外抗血小板凝集活性 

分 类 号：R914[医药卫生—药物化学]