Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3859-61. doi: 10.1016/s0960-894x(03)00708-x.

Abstract

A novel series of indole-2-carboxamide derivatives was prepared and identified as NR2B selective NMDA receptor antagonists. The influence of the number and position of OH groups on the indole skeleton as well as the substitution of the piperidine ring on the biological activity of the compounds was studied.

MeSH terms

  • Binding, Competitive / drug effects
  • Excitatory Amino Acid Antagonists / pharmacology
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Phenols / pharmacology
  • Piperidines / pharmacology
  • Radioligand Assay
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship

Substances

  • Excitatory Amino Acid Antagonists
  • Indoles
  • NR2B NMDA receptor
  • Phenols
  • Piperidines
  • Receptors, N-Methyl-D-Aspartate
  • Ro 25-6981