Pyridazinones as selective cyclooxygenase-2 inhibitors

Bioorg Med Chem Lett. 2003 Feb 24;13(4):597-600. doi: 10.1016/s0960-894x(02)01045-4.

Abstract

Pyridazinone was found to be an excellent core template for selective COX-2 inhibitors. Two potent, selective and orally active COX-2 inhibitors, which were highly efficacious in rat paw edema and rat pyresis models, have been obtained.

MeSH terms

  • Animals
  • Cell Line
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / pharmacokinetics*
  • Cyclooxygenase Inhibitors / pharmacology
  • Edema / drug therapy
  • Humans
  • Inhibitory Concentration 50
  • Isoenzymes / antagonists & inhibitors*
  • Membrane Proteins
  • Metabolic Clearance Rate
  • Prostaglandin-Endoperoxide Synthases
  • Pyridazines / chemical synthesis*
  • Pyridazines / pharmacokinetics
  • Pyridazines / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Pyridazines
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, rat