半乳糖苷三氮唑鹰嘴豆芽素A的合成与抗缺氧活性研究

目的设计合成半乳糖苷三氮唑鹰嘴豆芽素A并研究其抗缺氧活性。方法以半乳糖叠氮化物、炔丙基溴和鹰嘴豆芽素A为原料,利用＂Click＂化学方法将糖基化三氮唑药效基团引入鹰嘴豆芽素A分子结构中得到一种衍生物——半乳糖苷三氮唑鹰嘴豆芽素A,并通过小鼠常压密闭耐缺氧实验和化学物质中毒实验对其抗缺氧活性进行评价。结果产物结构经1H-NMR、IR、EI-MS和元素分析确认,半乳糖苷三氮唑鹰嘴豆芽素A能够显著延长不同缺氧状态下小鼠的存活时间,且活性优于乙酰唑胺（P〈0.05,P〈0.01）。结论本研究采取的合成半乳糖苷三氮唑鹰嘴豆芽素A的方法操作简便、条件温和、产率较高,而且该化合物表现出较高的抗缺氧活性。

Synthesis and Anti-Hypoxia Activity of Galactosyl-triazole Biochanin A

Objective To study the synthesis and anti-hypoxia activity of galactosyl-triazole biochanin A.Methods The pharmacophore of galactosyl-triazole biochanin A was induced into biochanin A molecular structure by ＂ Click＂ chemistry using the galactose,propargyl bromide and biochanin A as starting material,and the galactosyl-triazole biochanin A was obtained. The anti-hypoxic activity of the title compound was evaluated using the normobaric hypoxia and chemical poisoning tests in hypoxia mice. Results The structure was identified by 1H-NMR,IR,EI-MS and elemental analysis. Compared with those by Acetazolamide,galactosyl-triazole biochanin A could significantly prolong the survival time of mice in different hypoxia conditions with better anti-hypoxia activity of the compound（ P 〈0. 05,P〈0. 01）.Conclusion The synthetic method of the glycosyl-triazole biochanin A is simple with mild reaction conditions,but high yield and anti-hypoxic activity.