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ID: ALA1147594

Journal: Bioorg Med Chem Lett

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

Authors: Riendeau D, Salem M, Styhler A, Ouellet M, Mancini JA, Li CS.

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.

CiteXplore: 14980665

DOI: 10.1016/j.bmcl.2003.12.047