| 5-甲基-7,4’-二羟基异黄酮水溶性衍生物的合成及其抗缺氧活性 |
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| 引用本文： | 雷英杰,赵康.5-甲基-7,4’-二羟基异黄酮水溶性衍生物的合成及其抗缺氧活性[J].中国药物化学杂志,2003(5). |
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| 作者姓名： | 雷英杰 赵康 |
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| 作者单位： | 天津大学药物科学与技术学院，天津大学药物科学与技术学院 天津 300072，天津理工学院生物与化工学院，天津 300191，天津 300072 |
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| 摘 要： | 目的5-甲基-7,4’-二羟基异黄酮水溶性衍生物的合成及其抗缺氧活性的比较。方法三氟化硼-乙醚催化的“一锅法”工艺制备母体化合物1,并通过甲基化和磺化反应合成衍生物2～4,常压耐缺氧试验评价其活性。结果化合物3和4水溶性强,且抗缺氧作用等价于母体化合物。结论新合成的水溶性化合物3和4具有明显的抗缺氧活性。
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| 关 键 词： | 药物化学 制备 化学合成 5-甲基-7 4’-二羟基异黄酮衍生物 抗缺氧 |
Synthesis and anti-hypoxia activity of water soluble derivatives of 5-methyl-7, 4'-dihydroxyisoflavone |
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| LEI Ying-jie,ZHAO Kang.Synthesis and anti-hypoxia activity of water soluble derivatives of 5-methyl-7, 4''''-dihydroxyisoflavone[J].Chinese Journal of Medicinal Chemistry,2003(5). |
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| Authors: | LEI Ying-jie ZHAO Kang |
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| Abstract: | Aim To synthesize 5-methyl-7, 4'-dihydroxyisoflavone(1)and its three new derivatives and to e-valuate their anti-hypoxia activities. Methods Orcinol and p-hydroxyphenylacetic acid were used as the major reactants to obtain the target compounds by multi-step synthesis and their anti-hypoxia activities were e-valuated by the mice tests of resistance to low pressure hypoxia. Results Three derivatives(2-4), including two water soluble ones, were synthesized and compounds 3 and 4 are new compounds. Conclusion The two sulfonates derivatives(3 and 4) have the similar bioactivities, or even better in anti-hypoxia of rats besides their water-soluble properties. |
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| Keywords: | medicinal chemistry preparation chemical synthesis 5-methyl-7 4'-dihydroxyisoflavone derivatives anti-hypoxia |
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