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Journal of Antimicrobial Chemotherapy (2001) 48, 179-184
© 2001 The British Society for Antimicrobial Chemotherapy

Ferrocene-chloroquine analogues as antimalarial agents: in vitro activity of ferrochloroquine against 103 Gabonese isolates of Plasmodium falciparum

B. Pradinesa,*, T. Fusaia, W. Dariesa, V. Lalogeb, C. Rogiera, P. Milletc, E. Panconid, M. Kombilae and D. Parzya

a Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Bd C. Livon, Parc Le Pharo, BP 46, 13998 Marseille Armées, France; b Service Médical, 6ième Bataillon d'Infanterie de Marine, Libreville, Gabon; c Centre Labusquière, Université de Bordeaux II, Bordeaux, France; d Institut de Recherche Pierre Fabre, Labège Innopole, France; e Département de Parasitologie-Mycologie-Médecine Tropicale, Faculté de Médecine et des Sciences de la Santé, Libreville, Gabon

The in vitro activities of ferrochloroquine, chloroquine, quinine, mefloquine, halofantrine, amodiaquine, primaquine, atovaquone and artesunate were evaluated against Plasmodium falciparum isolates from children with uncomplicated malaria from Libreville (Gabon), using an isotopic, micro, drug susceptibility test. The IC50 values for ferrochloroquine were in the range 0.43–30.9 nM and the geometric mean IC50 for the 103 isolates was 10.8 nM (95% CI 8.6–13.5 nM), while the geometric means for chloroquine, quinine, mefloquine, amodiaquine and primaquine were 370 nM, 341 nM, 8.3 nM, 18.1 nM and 7.6 µM, respectively. Ferrochloroquine was active against P. falciparum isolates, 95% of which showed in vitro resistance to chloroquine. Weak positive significant correlations were observed between the responses to ferrochloroquine and that to chloroquine, amodiaquine and quinine, but too low to suggest cross-resistance. There was no significant correlation between the response to ferrochloroquine and those to mefloquine, halofantrine, primaquine, atovaquone or artesunate. Ferrochloroquine may be an important alternative drug for the treatment of chloroquine-resistant malaria.

* Corresponding author. Tel: +33-4-91-15-01-10; Fax: +33-4-91-15-01-64; E-mail: bruno.pradines{at}free.fr


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