| 宋明霞,邓先清.含哌嗪基团的芳氧乙酸酯类化合物的合成及其促学习记忆作用的研究[J].井冈山大学自然版,2016,(1):98-101 |
| 含哌嗪基团的芳氧乙酸酯类化合物的合成及其促学习记忆作用的研究 |
| SYNTHESIS AND EFFECTS ON LEARNING AND MEMORY FACILITATION OF PIPERAZINE-CONTAINED ARYLOXY ACETATE DERIVATIVES |
| 投稿时间：2015-11-01 修订日期：2015-12-01 |
| DOI：10.3969/j.issn.1674-8085.2016.01.020 |
| 中文关键词: 芳氧乙酸酯 哌嗪 学习记忆 水迷宫 |
| 英文关键词: aryloxy acetate Piperazine learning and memory water maze |
| 基金项目:江西省自然科学基金项目(20142BAB215022) |
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| 摘要点击次数: 10209 |
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| 中文摘要: |
| 目的 合成一系列2-[1-(2-吡啶) 乙氧基]乙酸2-[4-取代哌嗪]乙酯类化合物,对其促小鼠学习记忆作用进行研究。方法 将2-乙基吡啶进行NBS溴代反应,得到α-溴代2-乙基吡啶(2),化合物2与α-羟基乙酸乙酯反应得到芳氧乙酸乙酯(3),化合物3与1-取代-4-羟乙基哌嗪(5a-5g)进行酯交换得到目标化合物2-[1-(2-吡啶)乙氧基]乙酸2-[4-取代哌嗪]乙酯(6a-6g)。 挑选两个化合物6a和6d,对其进行小鼠水迷宫实验,评价其促小鼠学习记忆活性。结果 合成了一系列含哌嗪基团的芳氧乙酸酯类化合物,通过1H-NMR和红外光谱确证了其结构。结论 小鼠水迷宫实验结果表明化合物6a和6d对乙醇所致小鼠学习记忆再现困难具有明显改善作用(P <0.05)。 |
| 英文摘要: |
| Objective: To synthesize a series of 2-(4-(4-substituted) piperazin-1-yl) ethyl 2-(1-(pyridin-2-yl) ethoxy) acetates, and study its effects on learning and memory facilitation in mice. Methods: The compounds 2-(4-(4-substituted)piperazin-1-yl)ethyl 2-(1-(pyridin-2-yl)ethoxy)acetates (6a-6g) were prepared by using 2-ethylpyridine as the starting material, which reacted with NBS to obtain compound 2. Compound 2 treated by 2-hydroxyacetic acid ethyl ester to give compound 3. The reaction of intermediate 3 and compounds 5a-5g produced the targets 6a-6g. The effects of compounds 6a and 6d on learning and memory in mice were tested by using swimming maze test. Results: A series of piperazine-contained aryloxy acetates were designed and synthesized, and the structures of these compounds were confirmed by IR and 1H-NMR spectrum. Conclusion:The pharmacological results showed that compound 6a and 6d could significantly improve the aquired dysmnesia of mice caused by 400 mL/L ethanol (P<0.05). |
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