Chemistry:ELQ-300
ELQ-300 is an experimental antimalarial medication. It is the first entry in a new class of antimalarials known as 4-quinolone-3-diarylethers.[1]
ELQ-300 acts as an inhibitor of the mitochondrial cytochrome bc1 complex (complex III in the electron transport chain) - A mechanism shared with some of the most potent fungicides known, the strobilurins.[1] In preclinical studies with mice, ELQ-300 was found to be highly active against Plasmodium falciparum and Plasmodium vivax at all life cycle stages that play a role in the transmission of malaria, and to have good oral bioavailability.[1]
Due to issues with crystallization, ELQ-300 was turned into a prodrug known as ELQ-331. ELQ-331 and two other similar drug candidates are currently in development.[2]
References
- ↑ 1.0 1.1 1.2 Nilsen A (2013). "Quinolone-3-diarylethers: a new class of antimalarial drug". Science Translational Medicine 5 (177): 177ra37. doi:10.1126/scitranslmed.3005029. ISSN 1946-6234. PMID 23515079.
- ↑ "Error: no
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Further reading
- "NIH-Supported Researchers Identify New Class of Malaria Compounds" (Press release). U.S. National Institutes of Health. March 20, 2013. Archived from the original on March 24, 2013.
