Abstract
New 4-aminoquinoline-derived esterscontaining the redox-active ferrocenegroup brought
in by either ferrocenyfor-mic or 4-ferrocenylbutanoic acids weresynthesized and tested
in vitro for theirantiplasmodial activity. The results re-vealed that only esters derived
from fer-rocenylformic acid were active againstboth chloroquine (CQ)-resistant Dd2
andCQ-sensitive D10 strains of Plasmodium falciparum. However, none of theseshowed higher actvity than CQ against the sensitive strain.
Ester 16, which pos-sesses a butyl branch in the structure,was the most active of
all. With an IC50 of0.13 mM on the resistant strain, this esterpossessed 2.5-fold higher activity than
CQ(IC50 = 0.34 mM). All tested esters showedgood selectivity towards P. falciparum with indexes
higher than 60.
Key words
Antiplasmodial activity - Chloroquine - Cytotoxicity - Ferrocene - Plasmodium falciparum