| 6-[4-(取代胺基乙酰胺基苯基)]-4,5-二氢-3(2H)哒嗪酮类化合物的合成及其抗血小板聚集活性研究 |
| 投稿时间：2008-05-14 点此下载全文 |
| 引用本文：柴晓云,张晨曦,胡宏岗,赵庆杰,但志刚,邹燕,俞世冲,吴秋业.6-[4-(取代胺基乙酰胺基苯基)]-4,5-二氢-3(2H)哒嗪酮类化合物的合成及其抗血小板聚集活性研究[J].药学实践杂志,2008,(6):444~446,467 |
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| 基金项目:上海市长宁区科委科研项目(20054Y17001);上海市重点学科资助项目(B906). |
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| 中文摘要:目的:合成新的含有胺基的哒嗪酮类化合物,并研究其对抗血小板聚集活性的影响。方法:以乙酰基为连接片段,引入不同的取代胺基,设计合成未见报道的目标化合物8个,所有化合物均经过1H-NMR谱等确证;体外药理实验参考Born方法进行。结果:所有化合物都具有体外抑制血小板聚集的活性,其中化合物（1）,（3）和（8）的活性较强,化合物（3）的活性是MCI-154的6倍。结论:引入不同的取代胺基,对化合物抑制血小板聚集的活性有影响。 |
| 中文关键词:化学合成 哒嗪酮类 体外抗血小板聚集活性 |
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| Synthesis and antiplatelet aggregative activity of 6-[4-(substituted amino acetamido-phenyl)]-4,5-dihydro-3(2H)-pyridazinones |
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| Abstract:Objective:To synthesize new pyridazinone derivatives substituted by different amino groups.Methods:Eight target compounds were designed and synthesized by inletting different substituted amino groups connecting through the acetyl fragment.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 for the first time.The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent.Compounds（1）,（3）and（8）have better activeties;compound （3）showed a 6 times higher activity than that of MCI-154.Conclusion:Inletting different substituted amino groups can enhance the antiplatelet aggregation activity of the compounds. |
| keywords:chemical synthesis pyridazinones antiplatelet aggregative activity in vitro |
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