Mishra Raghav, da Cunha Xavier Jayze, Kumar Nitin, Krishna Gaurav, Dhakad Prashant Kumar, Dos Santos Helcio Silva, Bandeira Paulo Nogueira, Rodrigues Tigressa Helena Soares, Gondim Diego Romao, Ribeiro Walber Henrique Ferreira, da Silva Draulio Sales, Teixeira Alexandre Magno Rodrigues, Pereira Wandresa Francelino, Marinho Emmanuel Silva
Department of Pharmacy, Lloyd School of Pharmacy, Knowledge Park II, Greater Noida, Uttar Pradesh 201306, India.
Department of Biological Chemistry, Regional University of Cariri, Crato-CE, Brazil.
Med Chem. 2025;21(2):96-121. doi: 10.2174/0115734064318361240827072124.
Malaria continues to be the primary cause of mortality worldwide, and timely recognition and prompt intervention are crucial in mitigating adverse consequences. This review article aims to examine the effectiveness and structural characteristics of quinoline-based compounds as antimalarial agents. It specifically focuses on their therapeutic effects as well as potential prospects for exploring structure-activity relationship (SAR). In addition, this study aims to identify lead compounds that can efficiently battle multidrug-resistant forms of and .
A comprehensive review was conducted to evaluate the effectiveness of quinoline-based antimalarial medications in eradicating and . The mechanism of action and SAR of these compounds were analyzed.
Quinoline-based antimalarials demonstrated significant effectiveness in eliminating parasites, particularly in regions severely impacted by malaria, including Africa and Asia. These compounds were found to exhibit tolerance and immune-modulating properties, indicating their potential for more widespread utilization. The investigation identified various new quinoline compounds with improved antimalarial activity, including metal-chloroquine complexes, diaminealkyne chloroquines, and cinnamoylated chloroquine hybrids. This study explored different mechanisms by which these compounds interact with parasites, including their ability to accumulate in the parasite's acidic food vacuoles and disrupt heme detoxification. The derivatives demonstrated strong efficacy against chloroquine-resistant strains and yielded positive results.
Quinoline-based compounds represent a promising avenue for combating malaria due to their demonstrated efficacy against and parasites. Further research on their mechanisms of action and SAR could lead to the development of more effective antimalarial medications.
疟疾仍然是全球死亡的主要原因,及时识别和迅速干预对于减轻不良后果至关重要。这篇综述文章旨在研究喹啉类化合物作为抗疟药物的有效性和结构特征。它特别关注其治疗效果以及探索构效关系(SAR)的潜在前景。此外,本研究旨在确定能够有效对抗多药耐药形式的 和 的先导化合物。
进行了一项全面综述,以评估喹啉类抗疟药物在根除 和 方面的有效性。分析了这些化合物的作用机制和构效关系。
喹啉类抗疟药在消除 寄生虫方面显示出显著效果,特别是在受疟疾严重影响的地区,包括非洲和亚洲。发现这些化合物具有耐受性和免疫调节特性,表明它们有更广泛应用的潜力。该研究确定了各种具有改进抗疟活性的新型喹啉化合物,包括金属-氯喹配合物、二胺炔基氯喹和肉桂酰化氯喹杂化物。本研究探讨了这些化合物与寄生虫相互作用的不同机制,包括它们在寄生虫酸性食物泡中积累并破坏血红素解毒的能力。这些衍生物对氯喹耐药菌株显示出强大的疗效,并取得了积极成果。
喹啉类化合物因其对 和 寄生虫的已证实疗效,代表了对抗疟疾的一个有前景的途径。对其作用机制和构效关系的进一步研究可能会导致开发出更有效的抗疟药物。