糖基化三氮唑白杨素衍生物的合成与抗缺氧活性研究

doi:10.16333/j.1001-6880.2015.03.011

天然产物研究与开发 ›› 2015, Vol. 27 ›› Issue (3): 427-431.doi: 10.16333/j.1001-6880.2015.03.011

糖基化三氮唑白杨素衍生物的合成与抗缺氧活性研究

范小飞1,2，景临林1，马慧萍1，樊鹏程1，高荣敏1,2，贾正平1*

1 兰州军区兰州总医院药剂科，兰州 730050；2 兰州大学药学院，兰州 730000

出版日期:2015-03-30 发布日期:2015-04-07

Synthesis and Anti-hypoxic Activity of Glycosyltriazole Chrysin Derivatives

FAN Xiao-fei 1,2, JING Lin-lin1, MA Hui-ping 1, FAN Peng-cheng1, GAO Rong-ming1,2, JIA Zheng-ping 1*

1 Department of Pharmacy,Lanzhou General Hospital,Lanzhou Command of CPLA,Gansu Lanzhou 730050,China; 2 Department of Medicinal Chemistry,Lanzhou University,Gansu Lanzhou,730000,China

Online:2015-03-30 Published:2015-04-07

摘要/Abstract

摘要： 以叠氮糖、炔丙基溴和白杨素为原料，利用“Click chemistry”将糖基化三氮唑药效基团巧妙的引入白杨素分子结构中得到4种糖基化三氮唑白杨素衍生物，产物结构经¹H NMR、IR、ESI-MS和元素分析确认。并通过小鼠常压密闭耐缺氧模型对4个目标化合物的药理活性进行评价，均能不同程度的延长小鼠的存活时间，其中化合物1b和4b的活性优于乙酰唑胺。

关键词: 白杨素, 点击化学, 糖基化三唑, 抗缺氧活性

Abstract: Four glycosyltriazole chrysin derivatives were synthesized using glucose,propargyl bromide and chrysin as starting material via “click chemistry”.The structures of the synthesized derivatives were characterized by ¹H NMR,IR,ESI-MS and elemental analysis.The anti-hypoxic activities of the 4 synthesized compounds were examined using normobaric hypoxia model of mice.Compared to the model group,4 chrysin derivatives enhanced the survival time of mice under hypoxic environment.The anti-hypoxic activity of compound 1b and 4b was better than that of acetazolamide.

Key words: chrysin, click chemistry, glycosyltriazole, anti-hypoxic activity

中图分类号:

O629.9

范小飞1,2，景临林1，马慧萍1，樊鹏程1，高荣敏1,2，贾正平1*. 糖基化三氮唑白杨素衍生物的合成与抗缺氧活性研究[J]. 天然产物研究与开发, 2015, 27(3): 427-431.

FAN Xiao-fei 1,2, JING Lin-lin1, MA Hui-ping 1, FAN Peng-cheng1, GAO Rong-ming1,2, JIA Zheng-ping 1*. Synthesis and Anti-hypoxic Activity of Glycosyltriazole Chrysin Derivatives[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2015, 27(3): 427-431.

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糖基化三氮唑白杨素衍生物的合成与抗缺氧活性研究

Synthesis and Anti-hypoxic Activity of Glycosyltriazole Chrysin Derivatives

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