Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors

Bioorg Med Chem Lett. 1999 Apr 19;9(8):1171-4. doi: 10.1016/s0960-894x(99)00157-2.

Abstract

A series of sulfonamide-substituted 4,5-diarylthiazoles was prepared via three synthetic routes as selective COX-2 inhibitors. Recently in the synthesis of selective COX-2 inhibitors we have discovered that the sulfonamide moiety is a suitable replacement for the methylsulfonyl moiety yielding compounds with activity both in vitro and in vivo.

MeSH terms

  • Animals
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis
  • Humans
  • Isoenzymes / drug effects*
  • Membrane Proteins
  • Models, Chemical
  • Prostaglandin-Endoperoxide Synthases / drug effects*
  • Rats
  • Sulfonamides / chemistry*
  • Thiazoles / chemical synthesis*

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Sulfonamides
  • Thiazoles
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases