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2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基)环戊酮的合成及抗炎活性研究
引用本文:董金华,徐莉英,秦华,李莉,许丁元,计志忠. 2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基)环戊酮的合成及抗炎活性研究[J]. 药学学报, 1998, 33(7): 548-552
作者姓名:董金华  徐莉英  秦华  李莉  许丁元  计志忠
作者单位:沈阳药科大学,沈阳110015
摘    要: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.

关 键 词:环戊酮衍生物  Mannich碱  胺交换反应  抗炎活性
收稿时间:1997-08-20

SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF 2-(E)-(4-HYDROXY-3-METHOXYBENZYLIDENE)-5-(N-SUBSTITUTED AMINOMETHYL) CYCLOPENTANONES
J Dong,L Xu,H Qin,L Li,D Xu,Z Ji. SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF 2-(E)-(4-HYDROXY-3-METHOXYBENZYLIDENE)-5-(N-SUBSTITUTED AMINOMETHYL) CYCLOPENTANONES[J]. Acta pharmaceutica Sinica, 1998, 33(7): 548-552
Authors:J Dong  L Xu  H Qin  L Li  D Xu  Z Ji
Affiliation:Shenyang Pharmaceutical University, Shenyang 110015.
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.
Keywords:Mannich base  Amine exchange reaction  Antiinflammatory activity  Cyclopentanone derivative
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