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2-(E)-(4-羟基-3-甲氧基亚苄基)-5-(N-取代氨甲基)环戊酮的合成与抗炎活性

[Synthesis and antiinflammatory activity of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted aminomethyl) cyclopentanones].

作者信息

Dong J, Xu L, Qin H, Li L, Xu D, Ji Z

机构信息

Shenyang Pharmaceutical University, Shenyang 110015.

出版信息

Yao Xue Xue Bao. 1998 Jul;33(7):548-52.

PMID:12016891
Abstract

In search for new antiinflammatory agents, a series of 2-(E)-(4-hydroxy-3-methoxybenzylidene)-5-(N-substituted aminomethyl) cyclopentanones was synthesized via Stork reaction, Mannich reaction and amine exchange reaction. All of the fifteen target compounds were characterized by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several target compounds exerted appreciable effect on xylene-induced ear edema in mice and that alteration of the substituents of anilines showed significant influence on antiinflammatory potency.

摘要

为寻找新型抗炎药,通过斯托克反应、曼尼希反应和胺交换反应合成了一系列2-(E)-(4-羟基-3-甲氧基亚苄基)-5-(N-取代氨甲基)环戊酮。通过光谱分析和元素分析对所有15种目标化合物进行了表征。初步药理试验表明,几种目标化合物对二甲苯诱导的小鼠耳肿胀有明显作用,苯胺取代基的改变对抗炎效力有显著影响。

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