ABSTRACT

Background: In this study, some new 3-aryl, 2-substituted quinazoline-4(3H)-one of derivatives was synthesized using a threestep synthetic route to evaluate the antimalarial activity. To evaluate the in vivo antimalarial activities a four-day suppressive standard test was used, and the acute toxicity test was investigated using male Swiss Albino mice (20g each) according to reported methods for the synthesized compounds. The in vivo antimalarial activity of these compounds on P. berghei infected mice was found to be moderate to high at oral dose 0.04846 mmol/kg /day. This dose is equal to 25 mg/kg of chloroquine phosphate which cause 100% inhibition of the parasite. It is worth mentioning that most active compounds (E) -3 Phenyl -2- [2- (pyridine-4-yl) vinyl]-4(3H)-quinazolinone IVa (64.02%, (E)-2- [2-(4 -Hydroxy-3-methoxystyryl)-vinyl)-3-phenyl-4(3H)- quinazolinone IVc (77.25%) and (E)-2-[2-(Pyridin-4-yl)-vinyl]-3-phenenylamine-4(3H)- quinazolinone IVe (73.54%) showed a dose-dependent increase in present suppression in antimalarial activities. The results of acute toxicity indicated that all test compounds proved to be non-toxic and well tolerated by the experimental animals up to 300 mg/kg in oral and 140 mg/kg in parental studies. Keywords: Acute toxicity; Antimalarial; Plasmodium berghei; Quinazolin-4(3H)-one derivative
Publication date: 01/12/2021

https://ijbpas.com/pdf/2021/December/MS_IJBPAS_2021_DEC_SPCL_2061.pdf

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https://doi.org/10.31032/IJBPAS/2021/10.12.2061