The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1773-8. doi: 10.1016/s0960-894x(99)00288-7.

Abstract

The development of a COX-2 inhibitor rofecoxib (MK 966, Vioxx) is described. It is essentially equipotent to indomethacin both in vitro and in vivo but without the ulcerogenic side effect due to COX-1 inhibition.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • CHO Cells
  • Cricetinae
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemistry
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Indomethacin / adverse effects
  • Indomethacin / pharmacology
  • Inhibitory Concentration 50
  • Isoenzymes / chemistry*
  • Lactones / administration & dosage
  • Lactones / adverse effects
  • Lactones / chemical synthesis*
  • Lactones / pharmacology*
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / chemistry*
  • Rats
  • Sulfones

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Enzyme Inhibitors
  • Isoenzymes
  • Lactones
  • Membrane Proteins
  • Sulfones
  • rofecoxib
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, rat
  • Indomethacin