Design, Synthesis and In-Vivo Biological Activity Testing of 2, 3-DISUBSTITUTED 4(3H)-QUINAZOLINONE Derivatives as Anti-Malarial Agents (original) (raw)

2015

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-disubstituted4(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 antimalarial 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.

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