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]
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Preferred IUPAC name
6-Chloro-7-methoxy-2-methyl-3-{4-[4-(trifluoromethoxy)phenoxy]phenyl}quinolin-4(1H)-one | |
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C24H17ClF3NO4 |
Molar mass | 475.85 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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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]
References
- Nilsen A; et al. (2013). "Quinolone-3-diarylethers: a new class of antimalarial drug". Science Translational Medicine. 5 (177): 177ra37. doi:10.1126/scitranslmed.3005029. ISSN 1946-6234. PMC 4227885. PMID 23515079.
Further reading
- "NIH-Supported Researchers Identify New Class of Malaria Compounds" (Press release). U.S. National Institutes of Health. March 20, 2013.
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