Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors

Bioorg Med Chem Lett. 2001 May 21;11(10):1325-8. doi: 10.1016/s0960-894x(01)00212-8.

Abstract

The carboxyl group of the NSAID indomethacin was replaced with a variety of substituted thiazoles to obtain a series of potent, selective inhibitors of COX-2. Additional substitutions were made at the 1-position and 5-position of the indole of indomethacin.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / pharmacology
  • Humans
  • Indomethacin / analogs & derivatives*
  • Indomethacin / chemical synthesis
  • Indomethacin / pharmacology
  • Inhibitory Concentration 50
  • Isoenzymes / drug effects
  • Isoenzymes / metabolism*
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / drug effects
  • Prostaglandin-Endoperoxide Synthases / metabolism*
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / pharmacology*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Thiazoles
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Indomethacin