Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class

  • Bioorg Med Chem Lett. 1999 Jan 18;9(2):151-6. doi: 10.1016/s0960-894x(98)00705-7.
N Ouimet  1 ,  C C Chan ,  S Charleson ,  D Claveau ,  R Gordon ,  D Guay ,  C S Li ,  M Ouellet ,  D M Percival ,  D Riendeau ,  E Wong ,  R Zamboni ,  P Prasit
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada Inc., Pointe Claire-Dorval, Québec, Canada.
Abstract

Substituted heterocyclic analogs in the Flosulide class were investigated as potential selective cyclooxygenase-2 inhibitors. 6-(4-Ethyl-2-thiazolylthio)-5-methanesulfonamido-3H-isobe nzofuran-1-one 14 was found to be the optimal compound in the series with superior in vitro and in vivo activities.