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  • Title: Synthesis and in vitro antiplasmodial activity of quinoline-ferrocene esters.
    Author: N'Da DD, Breytenbach JC, Smith PJ, Lategan C.
    Journal: Arzneimittelforschung; 2011; 61(6):358-65. PubMed ID: 21827047.
    Abstract:
    New 4-aminoquinoline-derived esters containing the redox-active ferrocene group brought in by either ferrocenyformic or 4-ferrocenylbutanoic acids were synthesized and tested in vitro for their antiplasmodial activity. The results revealed that only esters derived from ferrocenylformic acid were active against both chloroquine (CQ)-resistant Dd2 and CQ-sensitive D10 strains of Plasmodium falciparum. However, none of these showed higher actvity than CQ against the sensitive strain. Ester 16, which possesses a butyl branch in the structure, was the most active of all. With an IC50 of 0.13 mM on the resistant strain, this ester possessed 2.5-fold higher activity than CQ (IC50 = 0.34 mM). All tested esters showed good selectivity towards P. falciparum with indexes higher than 60.
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