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ID: ALA1157175

Journal: Bioorg Med Chem

Title: Chemical and biological investigation of N-hydroxy-valdecoxib: An active metabolite of valdecoxib.

Authors: Erdélyi P, Fodor T, Varga AK, Czugler M, Gere A, Fischer J.

Abstract: The inhibition of cyclooxygenase enzymes plays an important role in the treatment of inflammatory diseases. N-Hydroxy-4-(5-methyl-3-phenylisoxazol-4-yl)benzenesulfonamide (3)-a primary metabolite of the highly selective COX-2 inhibitor valdecoxib-was synthesized and stabilized as its monohydrate (3a.H(2)O). The anti-inflammatory properties of 3a.H(2)O were investigated in carrageenan-induced edema and in acute and chronic pain models. Based on our biological investigation, we conclude that N-hydroxy-valdecoxib 3a is an active metabolite of valdecoxib.

CiteXplore: 18353655

DOI: 10.1016/j.bmc.2008.02.088