| （E）－1－取代芳基－2－（1H－苯并咪唑－1－基）乙酮取代苯腙类化合物的合成及其抑制血小板聚集作用 |
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| 引用本文： | 李科,刘超美,吴秋业,张应辉,涂学军.（E）－1－取代芳基－2－（1H－苯并咪唑－1－基）乙酮取代苯腙类化合物的合成及其抑制血小板聚集作用[J].中国药物化学杂志,1995(1). |
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| 作者姓名： | 李科 刘超美 吴秋业 张应辉 涂学军 |
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| 作者单位： | 第二军医大学药学院 |
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| 摘 要： | 对３２个（Ｅ）－１－取代芳基－２－（１Ｈ－苯并咪唑－１－基）乙酮取代苯腙类化合物初步体外药理测试结果表明，均有不同程度抑制ＴＸＡ２合成酶从而抑制花生四烯酸（ＡＡ）诱导的血小板聚集作用。化合物（２）活性最强，其活性以ＩＣ５０值相比，强于Ｄａｚｏｘｉｂｅｎ，化合物（３），（９），（１５），（２５）也有较强的抑酶活性。初步探讨了该类化合物构效关系。
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| 关 键 词： | TXA_2合成酶抑制剂 取代苯腙 |
The Inhibitory Action of Analogues of (E)-1-Substitued Aromatic Group-2-(1H-Benzimidazol-1-yl)Ethanone Substitued Phenyldrazones on Platelet Aggregation |
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| Li Ke,Liu Chaomei,Wu Qitiye,Zhang Yinghui,Tu Xuejun.The Inhibitory Action of Analogues of (E)-1-Substitued Aromatic Group-2-(1H-Benzimidazol-1-yl)Ethanone Substitued Phenyldrazones on Platelet Aggregation[J].Chinese Journal of Medicinal Chemistry,1995(1). |
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| Authors: | Li Ke Liu Chaomei Wu Qitiye Zhang Yinghui Tu Xuejun |
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| Abstract: | Results of preliminary pharmacological tests showed that all of the test compounds had activity against TXA2 synthetase,thus inhibiting platelet aggregation induced by AA in vitro with rabbits. Compound (2) was the most potent. Its activity was stronger than that of Dazoxiben in comparison with that of IC50. Compounds (3),(9),(15),(25) also had good activity. the change of group substitution on benzene would affect inhibitory activity to TXA2 synthetase. |
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| Keywords: | TXA_2 synthetase inhibitor Substituted phenylhydrazones |
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