Volume 6, number 1
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Design, Synthesis and Molecular Modeling Study of Quinazolin-4(3H) Ones With Potential Anti-Inflammatory Activity

Zakaria K. Abd El-Samii, Said A. El Feky, Hanan A. Abd El Fattah and Amany M.H. Ghanim  

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Zagazig University, Zagazig Egypt.

ABSTRACT: The present investigation is concerned with the synthesis of different 2-methyl-4(3H)-quinazolinones with the objective of discovering novel and potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by spectral and elemental analyses. Some of the obtained compounds were evaluated for their anti-inflammatory activity as well as gastric ulcerogenic effects. Results showed that 2-[2-methyl-4-oxo-3(H)-quinazolin-3-yl]-N-(4-chlorophenyl-2-thiaoxothiazol-3-yl) acetamide (11 b) showed higher anti-inflammatory activity in carageenan-induced rat paw edema test with low gastric ulcerogenicity compared with indomethacin. Furthermore, molecular modeling studies were performed in order to rationalize the obtained biological results.

KEYWORDS: 4(3H)Quinazolinone; anti-inflammatory; docking; COX-2

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El-Samii Z. K. A, El Feky S. A, El Fattah H. A. A, Ghanim A. M. H. Design, Synthesis and Molecular Modeling Study of Quinazolin-4(3H) Ones With Potential Anti-Inflammatory Activity. Biosci Biotechnol Res Asia 2009;6(1)
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El-Samii Z. K. A, El Feky S. A, El Fattah H. A. A, Ghanim A. M. H. Design, Synthesis and Molecular Modeling Study of Quinazolin-4(3H) Ones With Potential Anti-Inflammatory Activity. Biosci Biotechnol Res Asia 2009;6(1). Available from: https://www.biotech-asia.org/?p=7847

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