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 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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Journal articles
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Submitted on : Thursday, November 17, 2011 - 8:51:29 AM
Last modification on : Thursday, February 21, 2019 - 9:56:02 AM

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Faustine Dubar, G. Anquetin, Bruno Pradines, Daniel Dive, Jamal Khalife, et al.. Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. Journal of Medicinal Chemistry, American Chemical Society, 2009, 52 (24), pp.7954-7957. ⟨10.1021/jm901357n⟩. ⟨hal-00641967⟩

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