| 川芎嗪衍生物的设计、合成及抗血小板凝集活性研究 |
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| 引用本文： | 樊玲玲,李毅,吴晓芳,李永,张珏.川芎嗪衍生物的设计、合成及抗血小板凝集活性研究[J].化学通报,2018,81(6):543-547. |
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| 作者姓名： | 樊玲玲 李毅 吴晓芳 李永 张珏 |
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| 作者单位： | 贵州医科大学药学院 |
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| 基金项目： | 贵州省化学合成药物研发利用工程技术研究中心项目(黔科合[2016]平台人才5402)；贵州省普通高等学校药物化学工程研究中心项目(黔教合KY字[2014]219号)；贵州省卫生计生委科学技术(gzwjkj2016-1-050)；贵州省科技支撑计划项目（黔科合支撑[2017]2835）和贵州大学绿色农药与生物工程教育部重点实验室开放基金资助项目（2018GDGP0101）。 |
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| 摘 要： | 分别以川芎嗪(TMP)和邻苯二胺为起始原料,经KMn O4氧化、酯缩合、环化、还原等步骤合成了7个新型的川芎嗪衍生物,其结构经1H NMR、13C NMR及HRMS确证。并采用Born比浊法初步测试了化合物的体外抗血小板凝集活性。结果表明,化合物3和7对二磷酸腺苷(ADP)诱导的血小板凝集抑制率IC50分别为0.23mmol/L和0.27mmol/L,优于母体化合物川芎嗪(0.42mmol/L)。
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| 关 键 词： | 川芎嗪 衍生物 合成 抗血小板凝集活性 |
| 收稿时间： | 2017/12/8 0:00:00 |
| 修稿时间： | 2018/4/13 0:00:00 |
Synthesis and Anti-platelet Aggregation Activity Evaluation of Ligustrazine Derivatives |
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| Fan Lingling,Li Yi,Wu Xiaofang,Li Yong and Zhang Jue.Synthesis and Anti-platelet Aggregation Activity Evaluation of Ligustrazine Derivatives[J].Chemistry,2018,81(6):543-547. |
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| Authors: | Fan Lingling Li Yi Wu Xiaofang Li Yong and Zhang Jue |
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| Institution: | College of Pharmacy,Guizhou Medical University,College of Pharmacy,Guizhou Medical University,College of Pharmacy,Guizhou Medical University,College of Pharmacy,Guizhou Medical University,College of Pharmacy,Guizhou Medical University |
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| Abstract: | Using ligustrazine (TMP) and o-phenylenediamine as the ingredients, seven derivatives were synthesized via KMnO4 oxidation, esterification, cyclization and reduction. The structures were confirmed by 1HNMR, 13CNMR and HRMS. The in vitro anti-platelet aggregation activity of the target compounds have been preliminarily tested by the Born turbidimetric method, and the experimental results showed that compounds 3 (IC50=0.23mmol/L) and 7 (IC50=0.27mmol/L) have significant inhibitory activity of against adenosine diphosphate (ADP) induced platelet aggregation comparison with ligustrazine (IC50=0.42mmol/L). |
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| Keywords: | Ligustrazine Derivatives Synthesis Anti-platelet aggregation activity |
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