ELQ-300
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ELQ-300 is an experimental antimalarial medication. It is the first entry in a new class of antimalarials known as ''
4-quinolone 4-Quinolone is an organic compound derived from quinoline. It and 2-quinolone are the two most important parent (meaning simplified) quinolones. 4-Quinolone exists in equilibrium with a minor tautomer, 4-hydroxyquinoline (CAS#611-36-9). Aside ...
-3-diarylethers''. ELQ-300 acts as an inhibitor of the mitochondrial cytochrome ''bc''1 complex (complex III in the
electron transport chain An electron transport chain (ETC) is a series of protein complexes and other molecules that transfer electrons from electron donors to electron acceptors via redox reactions (both reduction and oxidation occurring simultaneously) and couples th ...
) - A mechanism shared with some of the most potent
fungicide Fungicides are biocidal chemical compounds or biological organisms used to kill parasitic fungi or their spores. A fungistatic inhibits their growth. Fungi can cause serious damage in agriculture, resulting in critical losses of yield, quality, ...
s known, the
strobilurins Strobilurins are a group of natural products and their synthetic analogs. A number of strobilurins are used in agriculture as fungicides. They are part of the larger group of QIs (Quinone outside Inhibitors), which act to inhibit the respiratory ch ...
. In preclinical studies with mice, ELQ-300 was found to be highly active against ''
Plasmodium falciparum ''Plasmodium falciparum'' is a Unicellular organism, unicellular protozoan parasite of humans, and the deadliest species of ''Plasmodium'' that causes malaria in humans. The parasite is transmitted through the bite of a female ''Anopheles'' mosqu ...
'' and '' Plasmodium vivax'' at all life cycle stages that play a role in the transmission of malaria, and to have good oral bioavailability.


References


Further reading

* Antimalarial agents 4-Quinolones Trifluoromethyl ethers Diphenyl ethers Hydroquinone ethers Chloroarenes {{antiinfective-drug-stub