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新型香豆素-3-氨基酰胺及其α-硫辛酸加合物的抗氧化和抗炎活性的合成与评价

Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.

作者信息

Melagraki Georgia, Afantitis Antreas, Igglessi-Markopoulou Olga, Detsi Anastasia, Koufaki Maria, Kontogiorgis Christos, Hadjipavlou-Litina Dimitra J

机构信息

Laboratory of Organic Chemistry, School of Chemical Engineering, National Technical University of Athens, Athens, Greece.

出版信息

Eur J Med Chem. 2009 Jul;44(7):3020-6. doi: 10.1016/j.ejmech.2008.12.027. Epub 2009 Jan 19.

Abstract

In the present work a series of novel coumarin-3-carboxamides and their hybrids with the alpha-lipoic acid were designed, synthesized and tested as potent antioxidant and anti-inflammatory agents. The new compounds were evaluated for their antioxidant activity, their activity to inhibit in vitro lipoxygenase and their in vivo anti-inflammatory activity. In general, the derivatives were generally found to present antioxidant and anti-inflammatory activities. Discussion is made based on the results for the structure-activity relationships in order to define the structural features required for activity.

摘要

在本研究中,设计、合成并测试了一系列新型香豆素-3-羧酰胺及其与α-硫辛酸的杂化物,作为有效的抗氧化剂和抗炎剂。对新化合物的抗氧化活性、体外抑制脂氧合酶的活性以及体内抗炎活性进行了评估。总体而言,这些衍生物通常具有抗氧化和抗炎活性。基于这些结果对构效关系进行了讨论,以确定活性所需的结构特征。

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