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

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 a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-03, Vol.14 (5), p.1201-1203
Hauptverfasser:	RIENDEAU, Denis, SALEM, Myriam, STYHLER, Angela, OUELLET, Marc, MANCINI, Joseph A, CHUN SING LI
Format:	Artikel
Sprache:	eng
Schlagworte:	Alcohols - metabolism Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - metabolism Cyclooxygenase Inhibitors - pharmacology Drug Evaluation, Preclinical - methods Humans Isoenzymes - antagonists & inhibitors Isoenzymes - metabolism Medical sciences Membrane Proteins Pharmacology. Drug treatments Phenylpropionates - chemistry Phenylpropionates - metabolism Phenylpropionates - pharmacology Prostaglandin-Endoperoxide Synthases - metabolism
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.12.047