Synthesis and Biological Evaluation of New Quinoxaline Derivatives as Antioxidant and Anti-Inflammatory Agents.

Burguete, Asunción; Pontiki, Eleni; Hadjipavlou-Litina, Dimitra; Ancizu, Saioa; Villar, Raquel; Solano, Beatriz; Moreno, Elsa; Torres, Enrique; Pérez, Silvia; Aldana, Ignacio; Monge, Antonio

We report the synthesis, anti-inflammatory, and antioxidant activities of novel quinoxaline and quinoxaline 1,4-di- N-oxide derivatives. Microwave-assisted methods have been used to optimize reaction times and to improve yields. The tested compounds presented important scavenging activities and promising in vitro inhibition of soybean lipoxygenase (LOX). Two of the best LOX inhibitors (compounds and ) were evaluated as in vivo anti-inflammatory agents using the carrageenin-induced edema model. One of them (compound ) showed important in vivo anti-inflammatory effect (41%) similar to that of indomethacin (47%) used as the reference drug. Synthesis and Biological Evaluation of New Quinoxaline Derivatives as Antioxidant and Anti-Inflammatory Agents Asunción Burguete, Eleni Pontiki, Dimitra Hadjipavlou-Litina*, Saioa Ancizu, Raquel Villar, Beatriz Solano, Elsa Moreno, Enrique Torres, Silvia Pérez, Ignacio Aldana and Antonio Monge The synthesis, anti-inflammatory and antioxidant activities of new quinoxaline derivatives are reported. The new compounds exhibit important scavenging activities and promising values of in vitro inhibition of soybean LOX, One of them shows strong in vivo anti-inflammatory effect similar to that of indomethacin used as the reference drug.

QUINOXALINES; LIPOXYGENASES; ANTI-inflammatory agents; INDOMETHACIN; ANTIOXIDANTS

Chemical Biology & Drug Design, 2011, Vol 77, Issue 4, p255

1747-0277

Academic Journal

10.1111/j.1747-0285.2011.01076.x