Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors

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• 作者：Afshin Zarghi ; Tannaz Zebardast ; Bahram Daraie ; Mehdi Hedayati
• 关键词：1 ; 3-Benzthiazinan-4-ones ; COX-2 inhibition ; SAR
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2009
• 出版时间：1 August 2009
• 年：2009
• 卷：17
• 期：15
• 页码：5369-5373
• 全文大小：300 K

文摘

A new group of 1, 3-benthiazinan-4-ones, possessing a methyl sulfonyl 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-(p-fluoropheny)-2-(4-methylsulfonylphenyl)-1,3-benzthiazinan-4-one (7b) as a potent (IC₅₀ = 0.05 μM) and selective (selectivity index = 259) COX-2 inhibitor.