| 噻吩并四氢吡啶衍生物的合成及其抗血小板聚集活性研究 |
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| 引用本文： | Zhou YS,Wang PB,Liu Y,Chen JF,Yue N,Liu DK. 噻吩并四氢吡啶衍生物的合成及其抗血小板聚集活性研究[J]. 药学学报, 2011, 46(1): 70-74 |
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| 作者姓名： | Zhou YS Wang PB Liu Y Chen JF Yue N Liu DK |
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| 作者单位： | (1. 天津医科大学研究生院, 天津 300070; 2. 天津药物研究院, 天津 300193; 3. 天津工业大学环境与化学工程学院, 天津 300160) |
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| 基金项目： | 国家“重大新药创制”科技重大专项(2009ZX09103-078); 天津市科技计划项目(09ZCKFSH01300) |
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| 摘 要： | 为了寻找新型的ADP受体拮抗剂类抗血栓药物, 合成了18个未见文献报道的噻吩并四氢吡啶衍生物, 化合物结构经1H NMR和MS确证。大鼠体内抗血小板聚集活性研究表明, 化合物C1的活性优于阳性对照药噻氯匹定, 值得进一步深入研究; 化合物A4、B2、C4和C7均有不同程度的抑制血小板聚集的活性。
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| 关 键 词： | 噻吩并四氢吡啶衍生物 合成 ADP受体拮抗剂 抗血小板聚集 |
Synthesis of thienopyridine derivatives and its anti-platelet activity in vivo |
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| Zhou Yun-Song,Wang Ping-Bao,Liu Ying,Chen Ji-Fang,Yue Nan,Liu Deng-Ke. Synthesis of thienopyridine derivatives and its anti-platelet activity in vivo[J]. Acta pharmaceutica Sinica, 2011, 46(1): 70-74 |
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| Authors: | Zhou Yun-Song Wang Ping-Bao Liu Ying Chen Ji-Fang Yue Nan Liu Deng-Ke |
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| Affiliation: | ZHOU Yun-song1,2,WANG Ping-bao2,LIU Ying2,CHEN Ji-fang3,YUE Nan2,LIU Deng-ke2(1.Graduate School,Tianjin Medical University,Tianjin 300070,China,2.Tianjin Institute of Pharmaceutical Research,Tianjin 300193,3.School of Environmental and Chemical Engineering,Tianjin Polytechnic University,Tianjin 300160,China) |
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| Abstract: | To explore novel ADP receptor inhibitors with anti-thrombotic activity, eighteen compounds were synthesized and their structures were confirmed by 1H NMR and MS. The results showed that the activity of compound C1 was superior to ticlopidine in platelet aggregation inhibition tests in vivo and worthy for further investigation. Compounds A4, B2, C4 and C7 possessed moderate platelet aggregation inhibitory activities. |
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| Keywords: | thienopyridine derivative synthesis ADP receptor inhibitor anti-platelet aggregation |
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