Synthesis and Antimalarial Activity in Vitro and in Vivo of a New Ferrocene−Chloroquine Analogue
Journal of Medicinal Chemistry1997Vol. 40(23), pp. 3715–3718
Citations Over TimeTop 10% of 1997 papers
Christophe Biot, Guillaume Glorian, Lucien Maciejewski, Jacques Brocard, Olivier Domarle, Georgette Blampain, Pascal Millet, Alain Georges, Huguette Abessolo, Daniel Dive, Jacques Lébibi
Abstract
The antimalarial activities of ferrocenic compounds mimicking chloroquine and active upon chloroquine-resistant strains of Plasmodium falciparum were evaluated. Four 7-chloro-4-[[[2-[(N,N-substituted amino)methyl]ferrocenyl]methyl]amino]quinoline derivatives have been synthesized; one of them, 1a, showed high potent antimalarial activity in vivo on mice infected with Plasmodium berghei N. and Plasmodium yoelii NS. and was 22 times more potent against schizontocides than chloroquine in vitro against a drug-resistant strain of P. falciparum.
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