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, 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.
Biot
C
C
Laboratoire de Catalyse Hétérogène et Homogène, URA CNRS 402, Université des Sciences et Technologies, Villeneuve d'ASCQ, France.
Glorian
G
G
Maciejewski
L A
LA
Brocard
J S
JS
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002738:Chloroquine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D005260:Female; D005296:Ferrous Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D008288:Malaria / Q000097:blood / Q000188:drug therapy; D000075163:Metallocenes; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D010967:Plasmodium yoelii / Q000187:drug effects
D000962:Antimalarials; D005296:Ferrous Compounds; D000075163:Metallocenes; D002738:Chloroquine; C004998:ferrocene