A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors

  • Bioorg Med Chem Lett. 1999 Nov 15;9(22):3181-6. doi: 10.1016/s0960-894x(99)00559-4.
C S Li  1 ,  W C Black ,  C Brideau ,  C C Chan ,  S Charleson ,  W A Cromlish ,  D Claveau ,  J Y Gauthier ,  R Gordon ,  G Greig ,  E Grimm ,  J Guay ,  C K Lau ,  D Riendeau ,  M Thérien ,  D M Visco ,  E Wong ,  L Xu ,  P Prasit
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, Pointe-Clarie-Dorval, Quebec, Canada.
PMID: 10576684 DOI: 10.1016/s0960-894x(99)00559-4
Abstract

By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3fluorophenyl)-4-(4-methanesulfonylphenyl)-2 (5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in models of inflammation were obtained.