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

Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts
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DOI:
10.1016/j.ejmech.2008.12.027
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发表时间:
2009-07-01
影响因子:
6.7
通讯作者:
Hadjipavlou-Litina, Dimitra J.
Hadjipavlou-Litina, Dimitra J.
中科院分区:
医学1区
文献类型:
--
作者:
Melagraki, Georgia;Afantitis, Antreas;Hadjipavlou-Litina, Dimitra J.

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在本工作中,一系列新的香豆素-3-甲酰胺及其与α-硫辛酸的杂合物被设计、合成并测试为有效的抗氧化剂和抗炎剂。评价了新化合物的抗氧化活性、体外抑制脂氧合酶的活性和体内抗炎活性。一般来说,衍生物通常被发现呈现抗氧化和抗炎活性。根据构效关系的结果进行了讨论,以确定活性所需的结构特征。(C)2009年Elsevier Masson SAS。All rights reserved.
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. (C) 2009 Elsevier Masson SAS. All rights reserved.