苯并咪唑杂化衍生物的研究进展及其抗疟活性

W. Singh, B. Debnath, K. Manna
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引用次数: 0

摘要

疟原虫的一种寄生虫引起疟疾。这种寄生虫通过受感染蚊子的叮咬传播到社区。疟疾对常用抗疟药的耐药性是一个真正的人类健康问题。苯并咪唑衍生物对恶性疟原虫(P. falciparum)菌株具有广泛的抗疟活性。本文综述了苯并咪唑杂化衍生物的抗疟活性,并描述了其构效关系(SAR)和定量构效关系(QSAR)模型。系统综述了14篇论文。文献调查显示,新型苯并咪唑杂化衍生物能降低恶性疟原虫在肝脏和配子体阶段的活性,抑制血红素合成和β-血红素的形成。QSAR模型通过多元线性回归(MLR)和人工神经网络(ANN)来解释抗疟药即将发生的生长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Recent Trends in the Development of Benzimidazole Hybrid Derivatives and Their Antimalarial Activities
A parasite of the Plasmodium species initiates malaria. The parasite is transmitted to communities through the bite of an infected mosquito. Malarial resistance towards the commonly used antimalarial agents is a genuine human health problem. Benzimidazole derivatives exhibit a wide range of antimalarial activities against Plasmodium falciparum (P. falciparum) strain. The present review has summarized the antimalarial activity of benzimidazole hybrid derivatives and described its structural activity relationship (SAR) and quantitative structural-activity relationship (QSAR) model. A total of 14 papers were systematically reviewed. The literature survey has revealed that novel benzimidazole hybrid derivatives diminished the P. falciparum activity in the liver and gametocyte stages and inhibited heme synthesis and β-hematin formation. The QSAR models explain imminent antimalarial agent's growth through multiple linear regression (MLR) and artificial neural networks (ANN).
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