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  • Title: Design and synthesis of new 1,3-benzdiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
    Author: Zarghi A, Zebardast T, Hajighasemali F, Alipoor E, Daraie B, Hedayati M.
    Journal: Arch Pharm (Weinheim); 2012 Apr; 345(4):257-64. PubMed ID: 22076641.
    Abstract:
    A new group of regioisomeric 2,3-diaryl-1,3-benzdiazinan-4-ones, possessing a methyl sulfonyl pharmacophore, were synthesized and their biological activities were tested for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-(p-fluorophenyl)-2-(4-methylsulfonylphenyl)-1,3-benzdiazinane-4-one (2b) as a potent and highly selective (IC(50) = 0.07 µM; selectivity index = 572.8) COX-2 inhibitor.
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