Abstract
A NEW COMPOUND serves double duty in the fight against malaria. The dual-function molecule, based on an acridone scaffold, not only reverses resistance to quinoline antimalarial drugs such as chloroquine but also has antimalarial potency of its own ( Nature , DOI: 10.1038/nature07937). Acridones were previously shown to reverse resistance to antimalarials by sensitizing the malaria parasite to the drugs, but this is the first with intrinsic antimalarial properties. In addition to combating resistance to traditional and newer drugs, such as chloroquine and piperaquine, respectively, the new compound can kill the parasite on its own. Dubbed T3.5, the compound consists of a tricyclic acridone scaffold with a diethylamino side chain attached to the central nitrogen. This side chain provides a hydrogen-bond acceptor needed for the sensitization. Another nitrogen-containing side chain causes the molecule to accumulate in the parasite’s acidic digestive vacuole, the drug’s presumed site of action. T3.5’s antimal...
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