324761-30-0Relevant articles and documents
Synthesis and Antimalarial Activity of Trioxaquine Derivatives
Dechy-Cabarett, Odile,Benoit-Vical, Francois,Loup, Christophe,Robert, Anne,Gornitzka, Heinz,Bonhoure, Anne,Vial, Henri,Magnaval, Jean-Francoise,Seguela, Jean-Paul,Meunier, Bernard
, p. 1625 - 1636 (2007/10/03)
Trioxaquines are dual molecules that contain a trioxane motif linked to an aminoquinoline entity. Among the different compounds of this series, trioxaquine cis-15 (DU1302c), prepared from α-terpinene, a cheap natural product, showed efficient antimalarial activity in vitro on both sensitive and resistant strains of Plasmodium falciparum (IC50 = 5-19 nM). A stereochemical description of this stable, nontoxic, and non-genotoxic antimalarial agent is detailed. Mice infected with P. vinckei were successfully treated with cis-15 in a four-day suppressive test. The doses required to decrease parasitemia by 50% (ED50) were 5 and 18 mg kg -1d-1 after intraperitoneal and oral administration, respectively. Parasitemia clearance was complete without recrudescence at an intraperitoneal dose of 20 mgkg-1d-1.