European Journal of Biomedical and Pharmaceutical Sciences

DESIGN, SYNTHESIS AND IN-VIVO BIOLOGICAL ACTIVITY TESTING OF 2, 3-DISUBSTITUTED 4(3H)-QUINAZOLINONE DERIVATIVES AS ANTI-MALARIAL AGENTS

Gebisa Tuji Kefeni, Mohammed Hussen Bule*, Ariaya Hymete, Adnan A. Bekhit

ABSTRACT

The reaction of anthranilic acid with acetic anhydride produced acetanthranil. Further reacting the product with aromatic amines and aromatic aldehydes respectively produces a series of 2, 3-disubstituted-4(3H)-quinazolinone derivative. Compounds IVa-f were synthesized to investigate their anti-malarial activities. The in vivo anti-malarial activity of these compounds was tested on P.berghei infected mice at two doses (48.46 mol/kg/day and 96.92 mol/kg/day). Most active compounds IVa (64.02%), IVc (77.25%) and IVe (73.54%) showed a dose dependent increase in anti-malarial activities. Invivo acute toxicity studies of these compounds IVa-f indicates all to be non-toxic and well tolerated by the experimental animals up to 300 mg/ kg administered orally and 140mg/ kg administered parenterally. Therefore, test compounds IVa-f would represent a successful lead compound for the development of new class for anti-malarial agents.

Keywords: 4(3H)-quinazolinone, in vivo, anti-malarial, in vivo acute toxicity.