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Bioorg Med Chem. 2008 May 1;16(9):5322-30. doi: 10.1016/j.bmc.2008.02.088. Epub 2008 Mar 4.

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

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  • 1Medicinal Chemistry Research Laboratory No. IV., Gedeon Richter Plc., PO Box 27, H-1475 Budapest 10, Hungary. p.erdelyi@richter.hu

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.

PMID:
18353655
DOI:
10.1016/j.bmc.2008.02.088
[PubMed - indexed for MEDLINE]
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