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Synthesis, Biological Evaluation and Docking Studies of Novel Benzopyranone Congeners for Their Expected Activity as Anti-inflammatory, Analgesic and Antipyretic Agents by Amal A.M. Eissa; Nahla A.H. Farag; Gamal A.H. Soliman is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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a b s t r a c t 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. The synthesis of the pyrazole-containing new compounds 4 proved a successful hit; a

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Author

Amal A.M. Eissa; Nahla A.H. Farag; Gamal A.H. Soliman

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)