某些2,3-二取代-4(3H)-喹唑啉酮衍生物的体内抗疟活性评价
In vivo antimalarial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives.
作者信息
Birhan Yihenew Simegniew, Bekhit Adnan Ahmed, Hymete Ariaya
机构信息
Department of Chemistry, Natural and Computational Sciences College, Debre Markos University, P.O. Box 269, Debre Markos, Ethiopia.
Department of Pharmaceutical Chemistry, Alexandria University, Alexandria, 21215, Egypt.
出版信息
BMC Res Notes. 2015 Oct 20;8:589. doi: 10.1186/s13104-015-1578-x.
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.
背景
疟疾是一种被忽视的热带寄生虫病，影响着全球数十亿人。尽管近年来与疟疾相关的病例数和死亡人数在减少，但它仍是世界上最致命的疾病。本研究旨在调查一些2,3-二取代-4(3H)-喹唑啉酮衍生物的体内抗疟活性。
结果
使用4天抑制标准试验，在感染氯喹敏感的伯氏疟原虫ANKA株的小鼠中研究了受试化合物（6-9和11-13）的体内抗疟活性。受试化合物显示出显著的抗疟活性，平均抑制率为43.71-72.86%，显著高于阴性对照组（p<0.05）。化合物12和13在该组中表现出更好的抗疟活性，平均抑制率分别为67.60%和72.86%。
结论
受试化合物在感染伯氏疟原虫ANKA株的小鼠中显示出显著的体内抗疟活性。因此，3-芳基-2-（取代苯乙烯基）-4(3H)-喹唑啉酮是开发抗疟药物的一种可能的骨架。
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