N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists

Bioorg Med Chem Lett. 1999 Jan 18;9(2):249-54. doi: 10.1016/s0960-894x(98)00720-3.

Abstract

N-Substituted 5-aminomethylquinoxalinediones containing carboxy or phosphonic acids yield potent and selective AMPA and/or NMDA (glycine-binding site) antagonists. Phosphonic acid derivatives are particularly water-soluble and display potent anticonvulsant effects in the electroshock-induced convulsion assay in mice.

MeSH terms

  • Amino Acids / chemistry
  • Animals
  • Disease Models, Animal
  • Electroshock
  • Hydrobromic Acid / pharmacology
  • Hydrochloric Acid / pharmacology
  • Hydroxy Acids / chemistry
  • Inhibitory Concentration 50
  • Mice
  • N-Methylaspartate / antagonists & inhibitors*
  • Organophosphonates / chemistry
  • Organophosphonates / pharmacology*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology*
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / antagonists & inhibitors*

Substances

  • Amino Acids
  • Hydroxy Acids
  • Organophosphonates
  • Quinoxalines
  • Hydrobromic Acid
  • N-Methylaspartate
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
  • Hydrochloric Acid