Antimicrobial, anti-oxidant and hepatoprotective activities of Quinazolinone-4 derivatives on Paracetamol induced hepatotoxicity in Guinea pigs

ABSTRACT

In this study, 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 synthesis of new compounds in lab from 2-phenylbenzoxazinones-4 with some compound as [p-aminobenzenesulfonamides] in a medium of acid catalyst and strong polar aprotic solvents [DMSO and DMFA]. After purification and identification of the final synthesized products; known weight was dissolved in 1ml of DMSO. This solution was used to determine the antimicrobial activity, using diffusion method. Results showed that using of catalytic quantity of strong polar aprotic solvents increased the yield by 25% with DMSO and 12.5% with DMFA. A study of the in-vitro of compounds [A and B] shows no antibacterial activity. It is suggested that the activity will be shown clearly in experiments in vivo because these compounds will be metabolized into the corresponding sulfonamides. The synthesized compounds have been investigated for their toxicity and anti-oxidant activity [in vivo] by testing activity in inhibition of hepatotoxicity induced 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. In the anti-oxidant study, the investigated compounds A and B showed high anti-oxidant activity, [29.08% and 48.2% respectively] higher than the compared standard. It is concluded that that the new synthesized quinazolinone-4 derivatives are 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.