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

作　　者：董金华[1] 徐莉英[1] 秦华[1] 许丁元[1] 李莉[1] 计志忠[1] 

机构地区：[1]沈阳药科大学

出　　处：《Journal of Chinese Pharmaceutical Sciences》1998年第4期19-23,共5页中国药学（英文版）

摘　　要：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.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：Cyclopentanone derivative Mannich base Amine exchange reaction Anti  inflammatory activity 

分 类 号：R9[医药卫生—药学]