Synthesis and antimalarial activity of new quinazolinone-4 derivatives

In this study, we have two new compounds of quinazolinone-4 derivatives were synthesized and evaluated for some of their pharmacological activities that were predicted by computer program (PASS), and also testified for their yield obtained by using some of strong polar aprotic solvents.
The new compounds were synthesized in the lab by allowing interaction of 2-phenylbenzoxazinones-4 with p-aminobenzenesulfonamides in a medium of acid catalyst and strong polar aprotic solvents DMSO.In the pharmacological studies, the synthesized compounds have been investigated in vitro for their toxicity and antimalarial activity according to WHO method.
The pharmacological studies approved that the new compounds have low toxicity, since compound A  gave class VI (harmless) and compound B gave class V (practically non toxic) according to Sidorov’s classification. For the antimalarial activity, the investigated compounds (A&B) inhibit the maturation of ring form of plasmodium falciparum to schizont form.
We concluded from our study that the new synthesized quinazolinone-4 derivatives were preferably obtained with usage of strong polar aprotic solvents especially DMSO. In addition, the pharmacological investigations have confirmed the prediction of PASS that testifies the high reliability of the obtained results.