4.7 Article

Design and synthesis of novel quinolinone-3-aminoamides and their α-lipoic acid adducts as antioxidant and antiiflammatory agents

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 10, Pages 2450-2458

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm061173n

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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.

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