Title of article
Carbonic anhydrase; Scleractinian corals; Biomineralisation; Sulfonamide; Enzyme inhibitor; Secreted enzyme
Author/Authors
Amal A.M. Eissa، نويسنده , , Nahla A.H. Farag، نويسنده , , Gamal A.H. Soliman، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2009
Pages
12
From page
5059
To page
5070
Abstract
8-Acetyl-7-hydroxy-4-phenyl-2H-benzopyran-2-one as starting material a number of 8-substituted derivatives (i.e., hydrazones 2a,b, imine 2c, chalcones 3, pyrazoles 4, 3-cyano-2-oxo-dihydropyridines 5, and/or 3-cyano-2-imino-dihydropyridines 6) were synthesized and assayed for their anti-inflammatory, analgesic and antipyretic activities. Compounds 3c, 4b and 4i showed significant anti-inflammatory, analgesic and antipyretic activities. In addition, 1, 3b, 4d, 4e, 5b, 6a, 6c, 6d, 6e showed anti-inflammatory activity, 2b, 4h, 5e exhibit analgesic activity, and 2b, 4h, 5e showed antipyretic effect. In addition, molecular modeling and docking of the tested compounds into cyclooxygenase II complexed with its bound inhibitor indomethacin (4COX) using molsoft icm 3.4-8C program was performed in order to predict the affinity and orientation of the synthesized compounds at the active site. Also, it was found that the active compounds 1, 4i, 6a–e interact with both Serine 530, and Tyrosine 385 amino acids which are the main amino acids involved in the mechanism of cyclooxygenase II inhibition.
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2009
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306166
Link To Document