新型哒嗪酮衍生物的合成及其对血小板聚集的抑制作用
投稿时间:2013-06-11  修订日期:2013-10-16  点此下载全文
引用本文:宋琰,仓婕,孟蕾,马福家.新型哒嗪酮衍生物的合成及其对血小板聚集的抑制作用[J].药学实践杂志,2014,32(2):107~109,123
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作者单位E-mail
宋琰 解放军455医院药剂科, 上海 200052  
仓婕 解放军455医院药剂科, 上海 200052  
孟蕾 解放军455医院药剂科, 上海 200052  
马福家 解放军455医院药剂科, 上海 200052 fjma455@gmail.com 
中文摘要:目的 合成新的含有胺基的哒嗪酮类化合物,并研究其对此类化合物抗血小板聚集活性的影响。方法 设计合成未见报道的目标化合物9个,所有化合物均经过1H-NMR谱等确证;参考文献方法进行体外药理实验。结果 发现所有化合物都具有抗血小板凝集的活性,其中化合物 9c,9e 和 9i 的抗血小板凝集活性明显优于对照化合物MCI-154和CCI-17910。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
 
Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone
Abstract:Objective To study the antiplatelet aggregative activity of 6-(4-substitued acetamino-phenyl 4,5-dihydro-3(2H)-pyridazinones with different amino group. Methods Nine 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 not reported. The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent.Compounds 9c, 9e and 9i were better than MCI-154 and CCI-17910 in vitro. Conclusion Inletting different substituted amino groups could enhance the antiplatelet aggregation activity of the compounds.
keywords:chemical synthesis  pyridaziones  platelet aggregation
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