2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基) 环戊酮的合成及其抗炎活性研究

2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基) 环戊酮的合成及其抗炎活性研究

董金华, 徐莉英, 秦华, 许丁元, 李莉, 计志忠

沈阳药科大学, 沈阳 110015

收稿日期:1997-08-18 修回日期:1997-12-12 出版日期:1998-12-15 发布日期:1998-12-15

Synthesis and Anti-inflammatory Activity of 2-(E)-(4-Hydroxy-3-methoxybenzylidene)-5-(N-Substituted aminomethyl) Cyclopentanones

Jin-Hua Dong, Li-Ying Xu, Hua-Qin, Ding-Yuan Xu, Li Li, Zhi-Zhong Ji

Shenyang Pharmaceutical University, Shenyang 110015

Received:1997-08-18 Revised:1997-12-12 Online:1998-12-15 Published:1998-12-15

摘要/Abstract

摘要： 本文合成了15种2-(E)-(3-甲氧基-4-羟基苯亚甲基)环戊酮杂环胺Mannich碱盐酸盐和芳胺Mannich碱,并进行了初步的抗炎活性筛选。所有化合物结构均经波谱分析和元素分析证实。药理试验结果表明:部分化合物对二甲苯致小鼠耳肿胀有较显著的抑制作用; 苯胺取代基的变化对芳胺Mannich碱的抗炎活性有显著的影响。

关键词: 环戊酮衍生物, Mannich碱, 胺交换反应, 抗炎活性

Abstract: A series of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted ami-nomethyl) cyclopentanones was synthesized and evaluated for the anti-inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene-induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti-inflammatory potency.

Key words: Cyclopentanone derivative, Mannich base, Amine exchange reaction, Anti-inflammatory activity

Supporting:

董金华, 徐莉英, 秦华, 许丁元, 李莉, 计志忠. 2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基) 环戊酮的合成及其抗炎活性研究[J]. .

Jin-Hua Dong, Li-Ying Xu, Hua-Qin, Ding-Yuan Xu, Li Li, Zhi-Zhong Ji. Synthesis and Anti-inflammatory Activity of 2-(E)-(4-Hydroxy-3-methoxybenzylidene)-5-(N-Substituted aminomethyl) Cyclopentanones[J]. .

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