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2-(E)-亚苄基-5-芳氨基甲基环戊醇类化合物的合成及其抗炎活性研究
引用本文:邵太丽,MA Juan,滕伟,YU Zhi-ying,徐莉英,DONG Jin-hua.2-(E)-亚苄基-5-芳氨基甲基环戊醇类化合物的合成及其抗炎活性研究[J].中国药物化学杂志,2008,18(4):241-244.
作者姓名:邵太丽  MA Juan  滕伟  YU Zhi-ying  徐莉英  DONG Jin-hua
作者单位:1. 沈阳药科大学制药工程学院,辽宁,沈阳,110016;皖南医学院,药学系,安徽,芜湖,241002
2. 沈阳药科大学制药工程学院,辽宁,沈阳,110016
基金项目:高等学校博士学科点专项科研项目
摘    要:目的设计合成2-(E)-亚苄基-5-芳氨基甲基环戊醇类化合物,并对其抗炎活性进行初步的评价。方法以环戊酮为起始原料,通过Stork烯胺反应、Mannich缩合反应、胺交换反应和选择性还原制备目标化合物;以二甲苯致小鼠耳肿胀模型测试目标化合物的抗炎活性。结果共合成16个新化合物,其结构经^1H-NMR和MS谱确证。结论初步药理实验结果显示,4个目标化合物具有较强的抗炎活性。

关 键 词:2-(E)-亚苄基-5-芳氨基甲基环戊醇  选择性还原  抗炎活性
收稿时间:2008-2-28
修稿时间:2008-5-20

Synthesis and anti-inflammatory activity of 2-(E)-benzylidene-5-arylaminomethylcyclopentanols
SHAO Tai-li,MA Juan,TENG Wei,YU Zhi-ying,XU Li-ying,DONG Jin-hua.Synthesis and anti-inflammatory activity of 2-(E)-benzylidene-5-arylaminomethylcyclopentanols[J].Chinese Journal of Medicinal Chemistry,2008,18(4):241-244.
Authors:SHAO Tai-li  MA Juan  TENG Wei  YU Zhi-ying  XU Li-ying  DONG Jin-hua
Institution:(1.School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China;2. Department of Pharmacy, Wannan Medical College, Wuhu 241002, China;3. Pharmaceutical Department, Guangdong Food and Drug Vocational College, Guangzhou 510520, China)
Abstract:Abstract:Aim 2-(E)-benzylidene-5-aminomethylcyclopentanols were synthesized and their anti-inflammatory activity was studied. Methods The target compounds were synthesized from cyclopentanone via Stork reaction, Mannich condensation , amine exchange and selective reduction. Xylene-induced mice ear edema assay was used to evaluate their anti-inflammatory activity. Results Sixteen novel compounds were synthesized and characterized by 1H-NMR and MS . Conclusion Preliminary pharmacological test showed that four compounds possessed potent anti-inflammatory activity.
Keywords:2-benzylidene-5-arylaminomethylcyclopentanol  selective reduction  anti-inflammatory activity
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