| 6-［4-(取代哌嗪基)苯基］-4，5-二氢-3(2H)-哒嗪酮类化合物的合成及抑制血小板聚集作用 |
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| 引用本文： | 吴秋业,张广明,廖洪利.6-［4-(取代哌嗪基)苯基］-4，5-二氢-3(2H)-哒嗪酮类化合物的合成及抑制血小板聚集作用[J].中国药物化学杂志,1999,9(3). |
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| 作者姓名： | 吴秋业 张广明 廖洪利 |
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| 作者单位： | 第二军医大学药学院!上海200433(吴秋业，张广明，廖洪利，刘超美)，军事医学科学院六所!北京100850(吴波，倪瑾，李晓梅) |
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| 摘 要： | 根据哒嗪酮类化合物的构效关系和作用机制，以ＣＣＩ１７８１０ 为先导化合物，设计合成了１８ 个６［４（ 取代哌嗪基） 苯基］４，５二氢３（２ Ｈ）哒嗪酮类化合物．初步的体外药理试验表明：大部分目标化合物都有不同程度的抑制ＡＤＰ诱导的新西兰大白兔血小板聚集的作用，其中化合物（５）的活性最强，比先导化合物强５ 倍，化合物（６），（７） ，（１２） ，（１３） ，（１６） 的活性也比ＣＣＩ１７８１０ 强，并初步探讨了它们的构效关系．
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| 关 键 词： | 哒嗪酮 血小板聚集抑制剂 血小板聚集 |
Synthesis and Platelet Aggregation Inhibitory Activity of 6 [4 Substituted piperazinyl)phenyl] 4,5 Dihydro 3(2 H ) Pyridazinones |
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| Wu Qiuye,Zhang Guangming,Liao Hongli,Liu Chaomei.Synthesis and Platelet Aggregation Inhibitory Activity of 6 [4 Substituted piperazinyl)phenyl] 4,5 Dihydro 3(2 H ) Pyridazinones[J].Chinese Journal of Medicinal Chemistry,1999,9(3). |
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| Authors: | Wu Qiuye Zhang Guangming Liao Hongli Liu Chaomei |
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| Abstract: | Analogues of 6 (4 substituted piperazine)phenyl] 4,5 dihydro 3(2 H ) pyridazinones were synthesized in searching for more potent and selective antithrombotic drugs.All the title compounds were first reported.Results of the preliminary pharmacological tests showed that all compounds synthesized had activity against platelet aggregation induced by ADP in virto in rabbits.Compound (5) was the most potent.Compounds (6),(7),(9),(11) were more potent than CCI 17810 too. |
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| Keywords: | pyridazinones platelet aggregation inhibitor platelet aggregation |
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