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Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3.

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

Author information

1
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec, Canada H9H 3L1. denis_riendeau@merck.com

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.

PMID:
14980665
DOI:
10.1016/j.bmcl.2003.12.047
[Indexed for MEDLINE]

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