中文摘要：

目的设计合成一种新型氮氧自由基与γ-氨基丁酸偶联物并研究其抗缺氧活性。方法以对羟基苯甲醛、溴乙酸乙酯、γ-氨基丁酸甲酯盐酸盐和2,3-二甲基-2,3-二羟氨基丁烷为原料,经醚化、酰胺化、缩合和氧化反应得到一种氮氧自由基与γ-氨基丁酸的偶联物（化合物3）,并通过小鼠常压密闭耐缺氧实验对其抗缺氧活性进行评价。结果 3组在常压密闭缺氧实验下,与缺氧模型组比较,乙酰唑胺组和化合物3组存活时间均明显延长,差异有统计学意义（P〈0.01）,化合物3组与乙酰唑胺组比较存活时间延长（P〈0.01）。与正常对照组比较,缺氧模型组中LD含量显著升高（P〈0.01）,LDH活性显著降低（P〈0.01）;与缺氧模型组比较,化合物3组小鼠血浆中LD含量差异无统计学意义,但是LD累积速率明显降低,差异有统计学意义（P〈0.01）。结论氮氧自由基与γ-氨基丁酸偶联物的设计路线合理,合成方法简便,产率较高,并且表现出了较高的抗缺氧活性。

英文摘要：

Objective To design the synthesis of a nitronyl nitroxide-γ-aminobutyric acid conjugate and to investigate its anti-hypoxia activity. Methods A nitronyl nitroxide-γ-aminobutyric acid conjugate（ compound 3） was achieved via etherification,amidation,condensation and oxidizing reaction using 4-hydroxybenzaldehyde,ethyl bromoacetate,methyl 4-aminobutyrate hydrochloride and 2,3-dimethyl-2,3-dihydroxylamino butane as starting materials. The anti-hypoxic activities of the compound were evaluated using the normobaric hypoxia experiment of mice. Results Compared with those in the hypoxia model group,Acetazolamide and compound 3 groups had significantly prolonged survival time in the three groups under normobaric hypoxia experiment,and the differences were statistically significant（ P〈0. 01）. The survival time of mice in compound 3 group was significantly longer than that in Acetazolamide group（ P〈0. 01）. Compared with those in the normal control group,the lactic acid（ LD） content was significantly increased,while the l-lactate dehydrogenase（ LDH） activity was significantly decreased in compound 3 group（ P〈0. 01）. Compared with those in the hypoxia model group,the LD content had no significant changes,but the LD accumulation rate was significantly decreased in compound 3 group（ P〈0. 01）. Conclusion The synthetic route of the nitronyl nitroxide-γ-aminobutyric acid conjugate is rational and simple with high yield,and it exhibits excellent anti-hypoxic activity.