Synthesis and in vitro antiplasmodial activity of ferrocenyl aminoquinoline derivatives

• Ferrocenyl-4-aminoquinoline derivatives were prepared from 4,7-dichloroquinolines.
• Quinoline-based ferrocenes were tested for their antiplasmodial activity.
• Antiplasmodial activity was positively affected by the presence of the ferrocene moiety.

The aim of this study was to synthesize a series of ferrocenyl 4-aminoquinolines and to evaluate their activities against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquino-resistant). Some of the ferrocenyl compounds exhibited in vitro antiplasmodial activity in the nM range. In particular, (1R,4R)-N1-(7-chloroquinolin-4-yl)-N4-(ferrocenylmethyl)-N4-methylcyclohexane-1,4-diamine 17 presented the lowest IC50 value (26 nM) against CQ-resistant strains.

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