title: 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: Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, 20133 Milano, Italy.
authors: Michela
authors: M
authors: Bruno
authors: Beatrice
authors: B
authors: Trucchi
authors: Diego
authors: D
authors: Monti
authors: Sergio
authors: S
authors: Romeo
authors: Marcel
authors: M
authors: Kaiser
authors: Luisella
authors: L
authors: Verotta
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D001688:Biological Products / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D002460:Cell Line; D055808:Drug Discovery; D005260:Female; D016778:Malaria, Falciparum / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D051381:Rats
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D001572:Benzofurans; D001688:Biological Products; C073339:usnic acid; C039060:artenimol