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Design and Synthesis of Novel Quinolinone-3-aminoamides and Their α-Lipoic Acid Adducts as Antioxidant and Anti-inflammatory Agents

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journal contribution
posted on 17.05.2007, 00:00 by Anastasia Detsi, Dionysia Bouloumbasi, Kyriakos C. Prousis, Maria Koufaki, Giorgos Athanasellis, Georgia Melagraki, Antreas Afantitis, Olga Igglessi-Markopoulou, Christos Kontogiorgis, Dimitra J. Hadjipavlou-Litina
A series of N-substituted-quinolinone-3-aminoamides and their hybrids containing the α-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.