Trioxaferroquines as new hybrid antimalarial drugs.
The synthesis, characterization, and antimalarial evaluation of a new series of potential antimalarial molecules, named trioxaferroquines, are reported. Trioxaferroquines are hybrid antimalarial drugs containing a 1,2,4-trioxane covalently linked to ferroquine (Fq), a synthetic ferrocenylquinoline derivative currently under clinical development. The aim was to combine, within a single structure, an iron(II) species, a 1,2,4-trioxane, as in artemisinin, and a substituted quinoline, as in chloroquine.
Bellot
François
F
Laboratoire de Chimie de Coordination du CNRS, Toulouse, France.
Coslédan
Frédéric
F
Vendier
Laure
L
Brocard
Jacques
J
Meunier
Bernard
B
Robert
Anne
A
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004351:Drug Resistance; D004355:Drug Stability; D005260:Female; D005296:Ferrous Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008288:Malaria / Q000188:drug therapy; D000075163:Metallocenes; D051379:Mice; D008958:Models, Molecular; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
C503429:1,2,4-trioxane; D000634:Aminoquinolines; D000962:Antimalarials; D005296:Ferrous Compounds; D006571:Heterocyclic Compounds; D000075163:Metallocenes; C004998:ferrocene