title: Synthesis and biological evaluation studies of novel quinazolinone derivatives as antibacterial and anti-inflammatory agents.
abstract: Some novel 6,8-diiodo-2-methyl-3-substituted-quinazolin-4(3H)-ones bearing sulfonamide 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 considerable 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 compounds 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.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
authors.forename: Mohamed
authors.initials: M
authors.lastname: F Zayed
authors.affiliation: Department of Pharmacology and Toxicology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt ; Department of Pharmacy, College of Medical Rehabilitation Sciences, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.
authors.forename: Memy
authors.initials: M
authors.lastname: H Hassan
keywords: Anti-inflammatory; Antibacterial; Diiodo; Quinazolinone; Sulfonamides; Synthesis