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Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach

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Dubar, Faustine | Anquetin, G. | Pradines, Bruno | Dive, Daniel | Khalife, Jamal | Biot, Christophe

Edité par CCSD ; American Chemical Society -

International audience. 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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