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

Riendeau, Denis; Salem, Myriam; Styhler, Angela; Ouellet, Marc; Mancini, Joseph A; Li, Chun Sing

Riendeau, Denis; Salem, Myriam; Styhler, Angela; Ouellet, Marc; Mancini, Joseph A; Li, Chun Sing.

Affiliation

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

Bioorg Med Chem Lett ; 14(5): 1201-3, 2004 Mar 08.

Article in En | MEDLINE | ID: mdl-14980665

ABSTRACT

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.

Subject(s)

Cyclooxygenase Inhibitors/metabolism; Cyclooxygenase Inhibitors/pharmacology; Isoenzymes/antagonists & inhibitors; Phenylpropionates/metabolism; Phenylpropionates/pharmacology; Alcohols/metabolism; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors/chemistry; Drug Evaluation, Preclinical/methods; Humans; Isoenzymes/metabolism; Membrane Proteins; Phenylpropionates/chemistry; Prostaglandin-Endoperoxide Synthases/metabolism

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Collection: 01-internacional Database: MEDLINE Main subject: Phenylpropionates / Cyclooxygenase Inhibitors / Isoenzymes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2004 Document type: Article

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