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J Med Chem. 1997 Nov 7;40(23):3715-8.

Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue.

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  • 1Laboratoire de Catalyse Hétérogène et Homogène, URA CNRS 402, Université des Sciences et Technologies, Villeneuve d'ASCQ, France.

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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