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
Synthesis and antiplatelet aggregative activity of 6-[4-(substituted amino acetamido-phenyl)]-4,5-dihydro-3(2H)-pyridazinones
-
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。
-
关键词:
- 化学合成 /
- 哒嗪酮类 /
- 体外抗血小板聚集活性
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. -
点击查看大图
计量
- 文章访问数: 2322
- HTML全文浏览量: 140
- PDF下载量: 197
- 被引次数: 0
下载:
