Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach
Identifieur interne : 000086 ( Hal/Curation ); précédent : 000085; suivant : 000087Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach
Auteurs : Faustine Dubar [France] ; G. Anquetin [France] ; Bruno Pradines [France] ; Daniel Dive [France] ; Jamal Khalife [France] ; Christophe Biot [France]Source :
- Journal of Medicinal Chemistry [ 0022-2623 ] ; 2009-12-24.
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 chloroquinesusceptible 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.
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DOI: 10.1021/jm901357n
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<front><div type="abstract" xml:lang="en"> <p>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 chloroquinesusceptible 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.</p>
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<abstract xml:lang="en"> <p>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 chloroquinesusceptible 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.</p>
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