Raghav Mishra, Jayze da Cunha Xavier, Nitin Kumar, Gaurav Krishna, Prashant Kumar Dhakad, Helcio Silva Dos Santos, Paulo Nogueira Bandeira, Tigressa Helena Soares Rodrigues, Diego Romao Gondim, Walber Henrique Ferreira Ribeiro, Draulio Sales da Silva, Alexandre Magno Rodrigues Teixeira, Wandresa Francelino Pereira, Emmanuel Silva Marinho, Sucheta
{"title":"Exploring Quinoline Derivatives: Their Antimalarial Efficacy and Structural Features.","authors":"Raghav Mishra, Jayze da Cunha Xavier, Nitin Kumar, Gaurav Krishna, Prashant Kumar Dhakad, Helcio Silva Dos Santos, Paulo Nogueira Bandeira, Tigressa Helena Soares Rodrigues, Diego Romao Gondim, Walber Henrique Ferreira Ribeiro, Draulio Sales da Silva, Alexandre Magno Rodrigues Teixeira, Wandresa Francelino Pereira, Emmanuel Silva Marinho, Sucheta","doi":"10.2174/0115734064318361240827072124","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>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 <i>Plasmodium falciparum </i> and <i>Plasmodium vivax</i>.</p><p><strong>Methods: </strong>A comprehensive review was conducted to evaluate the effectiveness of quinoline-based antimalarial medications in eradicating <i>P. falciparum</i> and <i>P. vivax</i>. The mechanism of action and SAR of these compounds were analyzed.</p><p><strong>Results: </strong>Quinoline-based antimalarials demonstrated significant effectiveness in eliminating <i>P. falciparum</i> 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.</p><p><strong>Conclusion: </strong>Quinoline-based compounds represent a promising avenue for combating malaria due to their demonstrated efficacy against <i>P. falciparum</i> and <i>P. vivax</i> parasites. Further research on their mechanisms of action and SAR could lead to the development of more effective antimalarial medications.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":"21 2","pages":"96-121"},"PeriodicalIF":1.9000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115734064318361240827072124","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Objectives: 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 Plasmodium falciparum and Plasmodium vivax.
Methods: A comprehensive review was conducted to evaluate the effectiveness of quinoline-based antimalarial medications in eradicating P. falciparum and P. vivax. The mechanism of action and SAR of these compounds were analyzed.
Results: Quinoline-based antimalarials demonstrated significant effectiveness in eliminating P. falciparum 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.
Conclusion: Quinoline-based compounds represent a promising avenue for combating malaria due to their demonstrated efficacy against P. falciparum and P. vivax parasites. Further research on their mechanisms of action and SAR could lead to the development of more effective antimalarial medications.
期刊介绍：
Aims & Scope
Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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