In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives

2,3-二取代-4(3H)-喹唑啉酮衍生物的体内抗疟活性评价

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Abstract

BACKGROUND: Malaria is a neglected tropical parasitic disease affecting billons of people around the globe. Though the number of cases and deaths associated with malaria are decreasing in recent years, it is the most deadly disease in the world. This study aimed at investigating the in vivo antimalarial activities of some 2,3-disubstituted-4(3H)-quinazolinone derivatives. RESULTS: The in vivo antimalarial activities of the test compounds (6-9 and 11-13) were investigated using the 4-day suppressive standard test in mice infected with chloroquine-sensitive Plasmodium berghei ANKA strain. The tested compounds showed significant antimalarial activities with mean percentage suppression of 43.71-72.86 % which is significantly higher than the negative control group (p < 0.05). Compounds 12 and 13 displayed better antimalarial activities from the group with mean percentage suppression of 67.60 and 72.86 % respectively. CONCLUSION: The tested compounds showed significant in vivo antimalarial activities in mice infected with P. berghi ANKA strain. Thus, 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones represent a possible scaffold for the development of antimalarial agents.

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