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Original scientific paper

4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (EX15) and its Cu(II) Complex as New Oxicam Selective Cyclooxygenase-2 Inhibitors

Yousery El-Sayed Sherif ; Department of Chemistry, Faculty of Science and Arts, Olla, Taibah University, Kingdom of Saudi Arabia
Ahmed Abdel-Hamid El-Asmy ; Department of Chemistry, Faculty of Science, Mansoura University, Mansoura, Egypt
Mahmoud Lotfy ; Molecular Biology Department, Genetic Engineering and Biotechnology Research Institute, Minufiya University, Sadat City, Minufiya, Egypt

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4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (EX15) as nonsteroidal antiinflammatory drug (NSAIDs) of oxicam family has been synthesized bearing high se-lectivity for cyclooxygenase-2 (COX-2) inhibition and high ability to chelate with Cu(II) ions. The EX15-Cu(II) complex, and [Cu(EX15)(OAc)(H2O)2], were synthesized and characterized by using elemental analysis, spectral (UV-Vis, IR), conductance, thermal and magnetic studies. Two equations were predicted using quantitative structure activity relationship (QSAR) and regression analysis for the COX-2 and COX-1 selectivity (microsomal assay) with a regression correlation (R) close to unity. Two techniques were used to investigate the validity of these equations; macrophage cell line (in vitro) selectivity and collagen-adjuvant arthritis model in rats (in vivo) which showed a significant antioxidant, analgesic and antirheumatic effect for 4-hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide and its Cu(II) complex, [Cu(EX15)(OAc)(H2O)2]. (doi: 10.5562/cca1802)


Oxicam, metal complexes, analgesic, rheumatoid, anti-inflammatory

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