Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2

  • Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3. doi: 10.1016/j.bmcl.2003.12.047.
Denis Riendeau  1 ,  Myriam Salem ,  Angela Styhler ,  Marc Ouellet ,  Joseph A Mancini ,  Chun Sing Li
Affiliations
  • 1. Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec, Canada H9H 3L1. [email protected]
PMID: 14980665 DOI: 10.1016/j.bmcl.2003.12.047
Abstract

Loxoprofen, its trans-alcohol and cis-alcohol metabolites were evaluated for selectivity of inhibition of COX-2 over COX-1. The (2S,1'R,2'S)-trans-alcohol derivative was found to be the most active metabolite and to be a potent and nonselective inhibitor of COX-2 and COX-1 in both enzyme and human whole blood assays.

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