Synthesis and Biological Evaluation of Quinazolinone Derivatives as Antibacterial and Anti-Inflammatory Agents

Abstract Some novel 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones bearing sulfon- amide derivatives (4–11) were synthesized in good yields and evaluated for their possible antibacterial, anti-inflammatory activities and acute toxicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Their antibacterial activities were evaluated by the agar well diffusion method while their anti-inflammatory activities were evaluated by the carrageenan-induced hind paw edema test. All the tested compounds showed con- siderable antibacterial activities and high to moderate anti-inflammatory activities that last for 12 h compared to ibuprofen. All the tested compounds showed no toxic symptoms or mortality rates 24 h post-administration at tested anti-inflammatory doses. In addition, LD50 for all tested com- pounds was higher than that for ibuprofen implying their good safety margin. The obtained results showed that the most active compounds could be useful as a template for future design, modification and investigation to produce more active analogs.

Keywords— Quinazolinone derivatives, Antibacterial Agents, Anti-Inflammatory Agents, Compound Sturcture.

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Engineering Journal: Synthesis and Biological Evaluation of Quinazolinone Derivatives as Antibacterial and Anti-Inflammatory Agents

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