Synthesis and Antimalarial Activity in Vitro and in Vivo of a New Ferrocene−Chloroquine Analogue

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, s...

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Veröffentlicht in:Journal of medicinal chemistry 1997-11, Vol.40 (23), p.3715-3718
Hauptverfasser: Biot, Christophe, Glorian, Guillaume, Maciejewski, Lucien A, Brocard, Jacques S, Domarle, Olivier, Blampain, Georgette, Millet, Pascal, Georges, Alain J, Abessolo, Huguette, Dive, Daniel, Lebibi, Jacques
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container_end_page 3718
container_issue 23
container_start_page 3715
container_title Journal of medicinal chemistry
container_volume 40
creator Biot, Christophe
Glorian, Guillaume
Maciejewski, Lucien A
Brocard, Jacques S
Domarle, Olivier
Blampain, Georgette
Millet, Pascal
Georges, Alain J
Abessolo, Huguette
Dive, Daniel
Lebibi, Jacques
description 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.
doi_str_mv 10.1021/jm970401y
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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.</description><identifier>ISSN: 0022-2623</identifier><identifier>EISSN: 1520-4804</identifier><identifier>DOI: 10.1021/jm970401y</identifier><identifier>PMID: 9371235</identifier><identifier>CODEN: JMCMAR</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Animals ; Antibiotics. Antiinfectious agents. 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Med. Chem</addtitle><description>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.</description><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antimalarials - chemical synthesis</subject><subject>Antimalarials - pharmacology</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Chloroquine - analogs &amp; derivatives</subject><subject>Chloroquine - chemical synthesis</subject><subject>Chloroquine - pharmacology</subject><subject>Female</subject><subject>Ferrous Compounds - chemical synthesis</subject><subject>Ferrous Compounds - pharmacology</subject><subject>Malaria - blood</subject><subject>Malaria - drug therapy</subject><subject>Medical sciences</subject><subject>Metallocenes</subject><subject>Mice</subject><subject>Pharmacology. 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source American Chemical Society; MEDLINE
subjects Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarials - chemical synthesis
Antimalarials - pharmacology
Antiparasitic agents
Biological and medical sciences
Chloroquine - analogs & derivatives
Chloroquine - chemical synthesis
Chloroquine - pharmacology
Female
Ferrous Compounds - chemical synthesis
Ferrous Compounds - pharmacology
Malaria - blood
Malaria - drug therapy
Medical sciences
Metallocenes
Mice
Pharmacology. Drug treatments
Plasmodium berghei - drug effects
Plasmodium falciparum - drug effects
Plasmodium yoelii - drug effects
title Synthesis and Antimalarial Activity in Vitro and in Vivo of a New Ferrocene−Chloroquine Analogue
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