Abstract
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 selectivity for cyclooxygenase-2 (COX-2) inhibition and high ability to chelate with Cu(II) ions. The EX15Cu(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 collagenadjuvant 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-1,1dioxide and its Cu(II) complex, [Cu(EX15)(OAc)(H2O)2]. (doi: 10.5562/cca1802)
Highlights
Copper induces an inhibition of PGE2 synthetase leading to a shift in synthesis from the inflammatory PGE2 to anti-inflammatory PGF series.[1]
The anti-inflammatory activity of the clinically used antiarthritic agents could be attributed to the formation of copper complex in blood carrying it to the site of inflammation.[5]
PGE2 Estimation The new compound, EX15, copper acetate, piroxicam, and Cu (II) - EX15 complex were tested for their antiinflammatory effects against COX-2 using the in vitro macrophage-like cells (P388Dl)
Summary
4-Hydroxy-2-methyl-N-(2-thiazole)-2H-1,2-benzothiazine-3carboxamide-1,1-dioxide (EX15) and its Cu(II) Complex as. 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 selectivity for cyclooxygenase-2 (COX-2) inhibition and high ability to chelate with Cu(II) ions. The EX15Cu(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 collagenadjuvant 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-1,1dioxide and its Cu(II) complex, [Cu(EX15)(OAc)(H2O)2].
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