Journal of Medicinal Chemistry 2007-05-17

Design and synthesis of novel quinolinone-3-aminoamides and their alpha-lipoic acid adducts as antioxidant and anti-inflammatory agents.

Anastasia Detsi, Dionysia Bouloumbasi, Kyriakos C Prousis, Maria Koufaki, Giorgos Athanasellis, Georgia Melagraki, Antreas Afantitis, Olga Igglessi-Markopoulou, Christos Kontogiorgis, Dimitra J Hadjipavlou-Litina

Index: J. Med. Chem. 50 , 2450-8, (2007)

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Abstract

A series of N-substituted-quinolinone-3-aminoamides and their hybrids containing the alpha-lipoic acid functionality were designed and synthesized as potential bifunctional agents combining antioxidant and anti-inflammatory activity. The new compounds were evaluated for their antioxidant activity and for their ability to inhibit in vitro lipoxygenase as well as for their anti-inflammatory activity in vivo. In general, the derivatives were found to be potent antioxidant or anti-inflammatory agents. The results are discussed in terms of structure-activity relationships and an attempt is made to define the structural features required for activity.