Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor

Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10.

Abstract

Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies.

MeSH terms

  • Allosteric Regulation
  • Animals
  • Humans
  • Imidazoles / chemistry*
  • Microsomes, Liver / metabolism
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / pharmacology
  • Pyridones / chemistry*
  • Rats
  • Receptors, Metabotropic Glutamate / chemistry*
  • Receptors, Metabotropic Glutamate / metabolism
  • Static Electricity
  • Structure-Activity Relationship

Substances

  • Imidazoles
  • Pyridines
  • Pyridones
  • Receptors, Metabotropic Glutamate
  • metabotropic glutamate receptor 2
  • imidazole