Synthesis of a potent antimalarial agent through natural products conjugation.

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 IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.

• Authors: Michela Bruno, Beatrice Trucchi, Diego Monti, Sergio Romeo, Marcel Kaiser, Luisella Verotta
• Journal: ChemMedChem (ChemMedChem) Vol. 8 Issue 2 Pg. 221-5 (Feb 2013) ISSN: 1860-7187 [Electronic] Germany
• PMID: 23307699 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Antimalarials
• Artemisinins
• Benzofurans
• Biological Products
• usnic acid
• artenimol

Topics

• Animals
• Antimalarials (chemical synthesis, chemistry, therapeutic use)
• Artemisinins (chemical synthesis, chemistry, therapeutic use)
• Benzofurans (chemical synthesis, chemistry, therapeutic use)
• Biological Products (chemical synthesis, chemistry, therapeutic use)
• Cell Line
• Drug Discovery
• Female
• Malaria, Falciparum (drug therapy, parasitology)
• Mice
• Parasitic Sensitivity Tests
• Plasmodium falciparum (drug effects)
• Rats