| 吡考他胺类似物的合成及其抑制血小板聚集作用 |
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| 引用本文： | 刘秀杰,张凤霞,张立光,张晶,李桂珠,王保杰,邵英禄,方林,程卯生. 吡考他胺类似物的合成及其抑制血小板聚集作用[J]. 中国药物化学杂志, 2005, 15(6): 332-335 |
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| 作者姓名： | 刘秀杰 张凤霞 张立光 张晶 李桂珠 王保杰 邵英禄 方林 程卯生 |
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| 作者单位： | 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 |
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| 摘 要： | 目的为寻找新的抗血小板聚集剂,以抗血小板聚集药物吡考他胺(picotamide)为先导化合物,对其结构进行改造,合成新的类似物.方法以苯甲醚为原料,经3步反应制得中间体4-甲氧基-1,3-苯二甲酰氯,经与不同的胺类化合物进行取代反应制得目标化合物.结果与结论共制得10个新化合物,其结构经红外和核磁共振谱确证.药理实验结果表明,化合物PN9和PN10的抗血小板聚集活性很高,明显优于阳性对照药物picotamide.
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| 关 键 词： | 药物化学 化合物制备 化学合成 吡考他胺 血小板聚集抑制剂 |
| 文章编号： | 1005-0108（2005）06-0332-04 |
| 收稿时间： | 2005-05-31 |
| 修稿时间： | 2005-05-31 |
Synthesis and platelet aggregation inhibitory activities of the analogs of picotamide |
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| LIU Xiu-jie,ZHANG Feng-xia,ZHANG Li-guang,ZHANG Jing,LI Gui-zhu,WANG Bao-jie,SHAO Ying-lu,FANG Lin,CHENG Mao-sheng. Synthesis and platelet aggregation inhibitory activities of the analogs of picotamide[J]. Chinese Journal of Medicinal Chemistry, 2005, 15(6): 332-335 |
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| Authors: | LIU Xiu-jie ZHANG Feng-xia ZHANG Li-guang ZHANG Jing LI Gui-zhu WANG Bao-jie SHAO Ying-lu FANG Lin CHENG Mao-sheng |
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| Affiliation: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | Aim To search new antiplatelet aggregating agents, a series of novel compounds were synthesized through taking picotamide as lead compound. Method With 4-methoxy-1, 3-benzenedicarboxyl chloride and different arylamides as starting material, ten target compounds were synthesized. Results and conclusion The structures of ten novel compounds were confirmed by IR and ^1H-NMR spectroscopy and the activities in vitro of the compounds on antiplatelet aggregation were tested and assessed. Compounds PN9 and PN10 have significant antiplatelet aggregation activity, superior to that of the reference drug picotamide. |
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| Keywords: | medicinal chemistry compound preparation chemical synthesis picotamide antiplatelet aggregation |
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