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

…, G Anquetin, B Pradines, D Dive, J Khalife…

Index: Dubar, Faustine; Anquetin, Guillaume; Pradines, Bruno; Dive, Daniel; Khalife, Jamal; Biot, Christophe Journal of Medicinal Chemistry, 2009 , vol. 52, # 24 p. 7954 - 7957

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Citation Number: 54

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 ...