1. Academic Validation
  2. A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors

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

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, Pointe-Clarie-Dorval, Quebec, Canada.
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.

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