| 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 |
| 投稿时间：2008-04-14 点此下载全文 |
| 引用本文：孙亮,黄晓瑾,范颂杰,俞世冲,吴秋业.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[J].药学实践杂志,2008,(4):278~281 |
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| 基金项目:上海市长宁区科委资助课题(20054Y17001) |
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| 中文摘要: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1H-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。 |
| 中文关键词:合成 哒嗪酮类 体外抗血小板聚集活性 |
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| Synthesis and the antiplatelet aggregative activity of 6-(4-substituted acetamidophenyl)-4,5-dihydro-3(2H)-pyridazinones |
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| Abstract:Objective:To study the antiplatelet aggregative aclivity nf 6-（4-substituted acetamido-phenyl）-4,5-dihydro-3（2H）-py- ridazinones with different heterocylic groups.Methods:Ten target compounds were designed and synthesized.All of them were con- firmed 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 aggre- gative activity to a certain extent.Compound （5）,（9） and （10） were better than MCI-154 in vitro.Conclusion::The stereospecifie blockade and hydrophilieity of different heterocylic groups impacted the antiplatelet aggregative activity. |
| keywords:synthesis pyridazinones antiplatelet aggregation |
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