| 2-(E)-(4-甲基亚苄基)环戊酮曼尼希碱的合成及其抗炎活性研究 |
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| 引用本文： | 郎福双,徐莉英,董金华,王敏伟,计志忠.2-(E)-(4-甲基亚苄基)环戊酮曼尼希碱的合成及其抗炎活性研究[J].中国药物化学杂志,2002,12(3):130-133. |
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| 作者姓名： | 郎福双 徐莉英 董金华 王敏伟 计志忠 |
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| 作者单位： | 1. 沈阳药科大学制药工程学院,辽宁,沈阳,110016
2. 沈阳药科大学药学院,辽宁,沈阳,110016 |
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| 基金项目： | 国家自然科学基金项目 (39870 892 )，辽宁省教育厅高等学校科研基金项目 (2 0 15 10 4 7) |
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| 摘 要： | 目的 合成2－（E）－（4－甲基亚苄基）环戊酮的曼尼希碱及其类似物并研究目标化合物的抗炎作用。方法 以N－环戊烯基吗啉、4－甲基苯甲醛及多种胺类为原料合成目标化合物，并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13个新化合物，经IR，^1H-NMR和MS确证其结构；部分化合物对二甲苯致小鼠耳肿胀具有较强的抑制作用。结论 2－（E）－（4－甲基亚苄基）环戊酮曼尼希碱类化合物具有较强的抗炎活性。
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| 关 键 词： | 环戊酮衍生物 曼尼希碱 抗炎 合成 |
| 文章编号： | 1005-0108(2002)03-0130-04 |
Synthesis and antiinflammatory activity of the Mannich bases of 2-(E)-(4-methylbenzylidene)cyclopentanone |
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| LANG Fu shuang ,XU Li ying ,DONG Jin hua ,WANG Min wei ,JI Zhi zhong.Synthesis and antiinflammatory activity of the Mannich bases of 2-(E)-(4-methylbenzylidene)cyclopentanone[J].Chinese Journal of Medicinal Chemistry,2002,12(3):130-133. |
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| Authors: | LANG Fu shuang XU Li ying DONG Jin hua WANG Min wei JI Zhi zhong |
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| Institution: | LANG Fu shuang 1,XU Li ying 1,DONG Jin hua 1,WANG Min wei 2,JI Zhi zhong 1 |
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| Abstract: | Aim To design and synthesize the Mannich bases of 2 ( E ) (4 methylbenzylidene)cyclopentanone,and to study their antiinflammatory activity.Methods The target compounds were synthesized from N (1 cyclopenten 1 yl)morpholine, p methylbenzaldehyde and amines and were evaluated with the model of the xylene induced ear edema in mice.Results Thirteen new compounds were obtained and confirmed by the spectral detection.Several compounds exerted significant inhibitory effects on the xylene induced ear edema in mice.Conclusion The Mannich bases of 2 ( E ) (4 methylbenzylidene)cyclopentanone had appreciable antiinflammatory activity.Substituted methylene alpha to the carbonyl group was necessary for the antiinflammatory activity. |
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| Keywords: | cyclopentanone derivative Mannich base antiinflammation |
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