N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4599-603. doi: 10.1016/j.bmcl.2007.05.083. Epub 2007 May 31.

Abstract

It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.

MeSH terms

  • Analgesics / chemistry*
  • Analgesics / pharmacology*
  • Animals
  • Area Under Curve
  • Binding Sites
  • Models, Molecular
  • Molecular Structure
  • Pain / drug therapy
  • Protein Binding
  • Rats
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Sulfonamides / blood
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*

Substances

  • Analgesics
  • Receptors, N-Methyl-D-Aspartate
  • Sulfonamides