From pyrroles to pyrrolo[1,2-a]pyrazinones: a new class of mGluR1 antagonists

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1342-5. doi: 10.1016/j.bmcl.2005.11.049. Epub 2005 Dec 5.

Abstract

Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was developed through a cyclization of the C-2 position on the pyrrole N-1 nitrogen. The resulting pyrrolo[1,2-a]pyrazinones are potent and noncompetitive antagonists.

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Inhibitory Concentration 50
  • Molecular Structure
  • Pyrazines / chemistry*
  • Pyrazines / pharmacology*
  • Pyrroles / chemistry*
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate / metabolism
  • Structure-Activity Relationship

Substances

  • Pyrazines
  • Pyrroles
  • Receptors, Metabotropic Glutamate
  • metabotropic glutamate receptor type 1