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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。
Acetylimidazolidinone was used as the raw material to react with non-steroidal anti-inflammatory drugs aspirin and indomethacin respectively to synthesize acetylimidazolidinone derivatives. The effects of them on the learning and memory ability of mice were observed. The chemical structure was modified according to the mosaic theory. After halogenated and condensed, the target compound was synthesized. The behavior of mice was detected by water maze. Two new compounds, phenyl 2- (1-acetyl-2-imidazolone-3-carbonyl) acetate (Target Compound A), 1-acetyl- ) 5-methoxy-2-methyl-1H-indolyl) acetyl-) 2-imidazolidinone (target compound B) in 20.7%, 30.5% yield, respectively. In the water maze test, compared with the model group, the target compound A can make the mouse travel time shortened, the number of errors reduced. The synthesis method has the advantages of stable and reliable process, mild conditions, green raw material safety and simple operation, and the target compound A enhances the learning and memory ability of the mice.