title: Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
abstract: The derivatization of the fluoroquinolone ciprofloxacin greatly increases its antimalarial activity by combining bioorganometallic chemistry and the prodrug approach. Two new achiral compounds 2 and 4 were found to be 10- to 100-fold more active than ciprofloxacin against Plasmodium falciparum chloroquine-susceptible and chloroquine-resistant strains. These achiral derivatives killed parasites more rapidly than did ciprofloxacin. Compounds 2 and 4 were revealed to be promising leads, creating a new family of antimalarial agents.
authors.affiliation: Universite de Lille 1, CNRS UMR 8181, ENSCL,Villeneuve d'Ascq Cedex, France.
authors.forename: Faustine
authors.initials: F
authors.lastname: Dubar
authors.forename: Guillaume
authors.initials: G
authors.lastname: Anquetin
authors.forename: Bruno
authors.initials: B
authors.lastname: Pradines
authors.forename: Daniel
authors.initials: D
authors.lastname: Dive
authors.forename: Jamal
authors.initials: J
authors.lastname: Khalife
authors.forename: Christophe
authors.initials: C
authors.lastname: Biot
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology*; D000075163:Metallocenes; D010963:Plasmodium falciparum / Q000187:drug effects; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D005296:Ferrous Compounds; D000075163:Metallocenes; D011355:Prodrugs; D002939:Ciprofloxacin; C479230:ferroquine; C004998:ferrocene