Title of article
Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors Original Research Article
Author/Authors
Afshin Zarghi، نويسنده , , Tannaz Zebardast، نويسنده , , Bahram Daraie، نويسنده , , Mehdi Hedayati، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2009
Pages
5
From page
5369
To page
5373
Abstract
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.
Keywords
1 , 3-Benzthiazinan-4-ones , COX-2 inhibition , SAR
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2009
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306200
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