Synthesis and biological evaluation of new quinoxaline derivatives as antioxidant and anti-inflammatory agents

Chem Biol Drug Des. 2011 Apr;77(4):255-67. doi: 10.1111/j.1747-0285.2011.01076.x. Epub 2011 Feb 9.

Abstract

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 7b and 8f) were evaluated as in vivo anti-inflammatory agents using the carrageenin-induced edema model. One of them (compound 7b) showed important in vivo anti-inflammatory effect (41%) similar to that of indomethacin (47%) used as the reference drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / chemical synthesis*
  • Antioxidants / pharmacology*
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / pharmacology
  • Female
  • Lipoxygenase / metabolism
  • Male
  • Molecular Structure
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / chemistry
  • Quinoxalines / pharmacology*
  • Rats

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Enzyme Inhibitors
  • Quinoxalines
  • Lipoxygenase