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Keywords:

  • antiprotozoal agents;
  • drug discovery;
  • Mannich bases;
  • medicinal chemistry;
  • usnic acids
Thumbnail image of graphical abstract

Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC50 value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.