European Journal of Medicinal Chemistry 2009-07-01

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

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

Index: Eur. J. Med. Chem. 44 , 3020-6, (2009)

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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.