解放军医药杂志2015，Vol.27Issue(12)：1-4,20,5.DOI:10.3969/j.issn.2095-140X.2015.12.001
氮氧自由基与γ-氨基丁酸偶联物的设计合成与抗缺氧活性研究
A Study on Design, Synthesis and Anti-hypoxia Activity of Nitronyl Nitroxide-γ-aminobutyric Acid Conjugate
摘要
Abstract
Objective To design the synthesis of a nitronyl nitroxide-γ-aminobutyric acid conjugate and to inves-tigate its anti-hypoxia activity. Methods A nitronyl nitroxide-γ-aminobutyric acid conjugate ( compound 3 ) was a-chieved via etherification, amidation, condensation and oxidizing reaction using 4-hydroxybenzaldehyde, ethyl bromoace-tate, methyl 4-aminobutyrate hydrochloride and 2, 3-dimethyl-2, 3-dihydroxylamino butane as starting materials. The an-ti-hypoxic activities of the compound were evaluated using the normobaric hypoxia experiment of mice. Results Com-pared 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 signifi-cantly decreased in compound 3 group ( P<0. 01 ) . Conclusion The synthetic route of the nitronyl nitroxide-γ-ami-nobutyric acid conjugate is rational and simple with high yield, and it exhibits excellent anti-hypoxic activity.关键词
氮氧自由基/γ-氨基丁酸/设计合成/抗缺氧活性Key words
Nitronyl nitroxide/γ-aminobutyric acid/Design and synthesis/Anti-hypoxia activity分类
医药卫生引用本文复制引用
景临林,马慧萍,樊鹏程,何蕾,贾正平..氮氧自由基与γ-氨基丁酸偶联物的设计合成与抗缺氧活性研究[J].解放军医药杂志,2015,27(12):1-4,20,5.基金项目
国家自然科学基金项目( 81202458 ) （ 81202458 ）
全军医药科研"十二五"面上项目(CLZ12JA04) （CLZ12JA04）
甘肃省自然科学基金(1308RJYA06) （1308RJYA06）
中国博士后科学基金(2012M521926) （2012M521926）
