Literature DB >> 18353655

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

Péter Erdélyi1, Tamás Fodor, Agnes Kis Varga, Mátyás Czugler, Anikó Gere, János Fischer.   

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.

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Year:  2008        PMID： 18353655     DOI： 10.1016/j.bmc.2008.02.088

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  4 in total

Review 1.  Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.

Authors:  Sureshbabu Dadiboyena; Adel Nefzi
Journal:  Eur J Med Chem       Date:  2010-08-06       Impact factor: 6.514

2.  Development and Characterization of a Hydroxyl-Sulfonamide Analogue, 5-Chloro-N-[2-(4-hydroxysulfamoyl-phenyl)-ethyl]-2-methoxy-benzamide, as a Novel NLRP3 Inflammasome Inhibitor for Potential Treatment of Multiple Sclerosis.

Authors:  Chunqing Guo; Jacob W Fulp; Yuqi Jiang; Xia Li; Jeremy E Chojnacki; Jingde Wu; Xiang-Yang Wang; Shijun Zhang
Journal:  ACS Chem Neurosci       Date:  2017-07-13       Impact factor: 4.418

3.  tert-Butyl 3-(8-bromo-4H,10H-1,2-oxazolo[4,3-c][1]benzoxepin-10-yl)-2-methyl-1H-indole-1-carboxyl-ate.

Authors:  Ankur Trigunait; P Malathy; K Ramachandiran; P T Perumal; K Gunasekaran
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-07-17

Review 4.  Selective COX-2 Inhibitors: Road from Success to Controversy and the Quest for Repurposing.

Authors:  Afaf A El-Malah; Magdy M Gineinah; Pran Kishore Deb; Ahdab N Khayyat; Monika Bansal; Katharigatta N Venugopala; Anfal S Aljahdali
Journal:  Pharmaceuticals (Basel)       Date:  2022-07-03
  4 in total

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