Article ID Journal Published Year Pages File Type
1372603 Bioorganic & Medicinal Chemistry Letters 2009 4 Pages PDF
Abstract

A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-benzyl-2-(4-methylsulfonylphenyl)-1,3-thiazinan-4-one (11a) as a potent (IC50 = 0.06 μM) and selective (selectivity index >285) COX-2 inhibitor.

Graphical abstractThe design, synthesis and evaluation of a series of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, as potent and selective COX-2 inhibitors are described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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