In vitro antimalarial activity of a new organometallic analog, ferrocene-chloroquine.
The in vitro activities of new organometallic chloroquine analogs, based on 4-amino-quinoleine compounds bound to a molecule of ferrocene, were evaluated against chloroquine-susceptible, chloroquine-intermediate, and chloroquine-resistant, culture-adapted Plasmodium falciparum lineages by a proliferation test. One of the ferrocene analogs totally restored the activity of chloroquine against chloroquine-resistant parasites. This compound, associated with tartaric acid for better solubility, was highly effective. The role of the ferrocene in reversing chloroquine resistance is discussed, as is its potential use for human therapy.
Domarle
O
O
Centre International de Recherches Médicales de Franceville, Gabon. odomarle@cirmfvr.fr
Blampain
G
G
Agnaniet
H
H
Nzadiyabi
T
T
Lebibi
J
J
Brocard
J
J
Maciejewski
L
L
Biot
C
C
Georges
A J
AJ
Millet
P
P
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance; D005290:Ferric Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*
C111773:7-chloro-4-((2-(N,N-dimethylaminomethyl))-N-methylferrocenylamino)quinoline; D000962:Antimalarials; D005290:Ferric Compounds; D002738:Chloroquine