Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. doi: 10.1016/j.bmcl.2007.09.083. Epub 2007 Sep 29.

Abstract

We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Naphthyridines / chemical synthesis*
  • Naphthyridines / pharmacology*
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate / physiology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Naphthyridines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate