3,4,5-三甲氧基苯甲酰胺类化合物的合成及抗疲劳活性  

Synthesis of 3,4,5-Trimethoxybenzamides and Antifatigue Activities

作　　者：范於菟[1] 武祥龙[1] 潘亚磊[1] 翟远坤[1] 梅其炳[1,2] 

机构地区：[1]西北工业大学生命学院 空间生物实验模拟技术国防重点学科实验室,陕西西安710072 [2]中国医药工业研究总院上海医药工业研究院,上海200437

出　　处：《中国医药工业杂志》2014年第4期312-314,共3页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金资助项目(21202130)

摘　　要：3,4,5-三甲氧基苯甲酸与三氟乙酸琥珀酰亚胺酯反应生成活性中间体,再与含氮杂环缩合得到3,4,5-三甲氧基苯甲酰胺化合物1a^1e。以小鼠负重游泳实验模型评价目标化合物的抗疲劳活性,并测定对大鼠大脑皮质AMPA受体结合的半数抑制浓度IC50值,结果显示1a、1b具有较好的抗疲劳活性且与AMPA受体结合力较强。A series ofnoval AMPA receptor modulators, 3,4,5-trimethoxybenzamides （1a - 1e）, were synthesized by the esterfication of 3,4,5-trimethoxy benzoic acid with N-succinimidyl-trifluoroacetate, then reacted with nitrogen heterocyclic rings. The antifatigue activities were evaluated by weight-loaded forced swimming test and AMPA receptor binding assay. The results showed that la and lb had potent antifatigue activities. Meanwhile, 1a and 1b also had high affinity with AMPA receptor.

关 键 词：AMPA受体调节剂 3 4 5-三甲氧基苯甲酰胺 合成 抗疲劳活性 

分 类 号：R979.1[医药卫生—药品]