乙酰基咪唑烷酮衍生物的合成及其对小鼠学习记忆能力的影响  

Synthesis of acetyl derivatives of imidazolidin and their effect on learning and memory capacities of mice

作　　者：田宝勇[1] 刘英华[1] 杜秀芳[2] 张忠敏[2] 王伟[2] 

机构地区：[1]河北科技大学河北省分析测试研究中心,河北石家庄050018 [2]河北医科大学药学院,河北石家庄050017

出　　处：《河北科技大学学报》2012年第1期27-31,共5页Journal of Hebei University of Science and Technology

基　　金：河北省科学技术研究与发展计划项目(07276101D-26)

摘　　要：以乙酰基咪唑烷酮为原料,分别与非甾体抗炎药阿司匹林、吲哚美辛反应,合成乙酰基咪唑烷酮衍生物,并观察其对小鼠学习和记忆能力的影响。根据拼合原理(mosaic theory)进行化学结构修饰,经卤代、缩合,合成目标化合物,应用水迷宫法检测小鼠行为学变化。合成了2个新化合物2-(1-乙酰基-2-咪唑酮-3-羰基)乙酸苯酯(目标化合物A),1-乙酰基-3-(2-(1-(4-氯-)5-甲氧基-2-甲基-1H-吲哚基)乙酰基-)2-咪唑烷酮(目标化合物B),产率分别为20.7%,30.5%。在水迷宫实验中,与模型组比较,目标化合物A可使小鼠游全程时间缩短,错误次数减少。合成方法工艺稳定可靠,条件温和,原料绿色安全,操作简单,目标化合物A对小鼠的学习、记忆能力有增强作用。Acetyl derivatives of imidazolidin were prepared by the reaction of acetyl imidazolidin with aspirin and indomethacin,non-steroidal anti-inflammatory drugs,respectively.Then their effect on the learning and memory function of mice is studied.According to mosaic theory to modify the chemcial constitution,the target compound was synthesized by halogenation and condensation reaction.After that,the praxiological changes of each group of mice are analyzedl by adopting the means of morris water maze.Two new compounds are obtained:2-(1-acetyl-2-oxoimidazol-idine-3-carbonyl)phenyl acetate(the target compound A)and 1-acetyl-3-(2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetyl)imidazolidin-2-one(the target compound B),with yield of 20.7% and 30.5%.The target compound A could shorten the time for swimming the whole process and decrease the times of mistakes compared with the model group in the Morris Water Maze tests.The process is stable,safe and free from pollution in mild condition.The target compound A is beneficial to increase the learning and memory capacities of mice.

关 键 词：乙酰基咪唑烷酮 拼合 合成 小鼠 学习和记忆 

分 类 号：R91[医药卫生—药学]