期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 15, 页码 5369-5373出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.06.056
关键词
1,3-Benzthiazinan-4-ones; COX-2 inhibition; SAR
资金
- Shahid Beheshti University
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 (IC(50) = 0.05 mu M) and selective (selectivity index = 259) COX-2 inhibitor. (C) 2009 Elsevier Ltd. All rights reserved.
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