Title:Exploring Quinoline Derivatives: Their Antimalarial Efficacy and Structural Features
Volume: 21
Issue: 2
Author(s): Raghav Mishra*, Jayze da Cunha Xavier*, Nitin Kumar, Gaurav Krishna, Prashant Kumar Dhakad, Hélcio Silva dos Santos, Paulo Nogueira Bandeira, Tigressa Helena Soares Rodrigues, Diego Romão Gondim, Walber Henrique Ferreira Ribeiro, Draulio Sales da Silva, Alexandre Magno Rodrigues Teixeira, Wandresa Francelino Pereira, Emmanuel Silva Marinho and Sucheta
Affiliation:
- 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
Keywords:
Quinoline derivatives, malaria, Plasmodium, antimalarial, structure-activity relationship, detoxification.
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.
