Abstract
Available anti-malarial tools have over the ten-year period prior to 2012 dramatically reduced the number of fatalities due to malaria from one million to less than six-hundred and thirty thousand. Although fewer people now die from malaria, emerging resistance to the first-line anti-malarial drugs, namely artemisinins in combination with quinolines and arylmethanols, necessitates the urgent development of new anti-malarial drugs to curb the disease. The quinolones are a promising class of compounds, with some demonstrating potent in vitro activity against the malaria parasite. This review summarizes the progress made in the development of potential anti-malarial quinolones since 2008. The efficacy of these compounds against both asexual blood stages and other stages of the malaria parasite, the nature of putative targets, and a comparison of these properties with anti-malarial drugs currently in clinical use, are discussed.
Highlights
Malaria represents a significant global health threat, with 40% of the world’s population being at risk of contracting this disease
Malaria arises from the invasion of red blood cells (RBCs) by a protozoan of the genus, Plasmodium [3]
Recent research involving the evaluation of anti-malarial properties of quinolones, indicates that these compounds demonstrate promising potential
Summary
Malaria represents a significant global health threat, with 40% of the world’s population being at risk of contracting this disease. Recent research involving the evaluation of anti-malarial properties of quinolones, indicates that these compounds demonstrate promising potential They show very good efficacies and target more than one stage of the malaria parasite life cycle, including the blood, liver and gametocyte stages. The acridinone (23, Figure 6) is an example of such an analogue It exhibits extraordinarily strong anti-malarial activity in vitro, with IC50 values of 1 pM against both the D6 and Dd2 strains of P. falciparum. Ethyl 2-(1,3-benzodioxol-5-yl)-7-methoxy-4-oxo-1,4dihydroquinoline-3-carboxylate (TDR 42098) This compound demonstrates improved potency against the blood stages of the CQ-R K1 and CQ-S NF54 strains of P. falciparum, and has better physicochemical properties, than endochin analogues, bearing a lipophilic side chain [43].
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