Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9. doi: 10.1016/j.bmcl.2007.07.047. Epub 2007 Aug 6.

Abstract

A novel series of potent 2-aryl pyrido[2,3-d]pyrimidine mGlu5 receptor antagonists are described. The synthesis and pharmacological activities of these analogs are discussed.

MeSH terms

  • Animals
  • CHO Cells
  • Calcium / metabolism
  • Cricetinae
  • Cricetulus
  • Cyclooxygenase 2 Inhibitors / therapeutic use
  • Excitatory Amino Acid Antagonists / chemical synthesis*
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Indicators and Reagents
  • Joints / pathology
  • Lactones / therapeutic use
  • Osteoarthritis / chemically induced
  • Osteoarthritis / drug therapy
  • Osteoarthritis / pathology
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Sulfones / therapeutic use

Substances

  • Cyclooxygenase 2 Inhibitors
  • Excitatory Amino Acid Antagonists
  • Indicators and Reagents
  • Lactones
  • Pyridines
  • Pyrimidines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate
  • Sulfones
  • rofecoxib
  • 6-methyl-2-(phenylethynyl)pyridine
  • Calcium