Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.
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.
Melagraki
Georgia
G
Laboratory of Organic Chemistry, School of Chemical Engineering, National Technical University of Athens, Athens, Greece.
Afantitis
Antreas
A
Igglessi-Markopoulou
Olga
O
Detsi
Anastasia
A
Koufaki
Maria
M
Kontogiorgis
Christos
C
Hadjipavlou-Litina
Dimitra J
DJ
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D003374:Coumarins / Q000737:chemistry*; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D008084:Lipoxygenase / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D051381:Rats; D013025:Glycine max / Q000201:enzymology; D008063:Thioctic Acid / Q000737:chemistry*
D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D003374:Coumarins; D016859:Lipoxygenase Inhibitors; D008063:Thioctic Acid; C030123:coumarin; D008084:Lipoxygenase