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.
Inhibitory zone diameters in mm; conc of standard 50 μg/ml, compounds 100 μg/ml.
LD50: dose that kills 50% of animals within 24 h after drug administration.
ED50 is the dose required to induce 50% inhibition of rat paw edema (50% anti-inflammatory effect).
ED50 was calculated using instate program by plotting results at all doses levels; Ibuprofen was tested at a dose range from 25 to 100 mg/kg and tested compounds from 25 to 200 mg/kg.
Footnotes
Peer review under responsibility of King Saud University.
