Synthesis and in vitro antiplasmodial activity of ferrocenyl aminoquinoline derivatives.

Eur J Med Chem

Université Lille Nord de France, Université de Lille 1, Unité de Catalyse et de Chimie du Solide, UMR CNRS 8181, ENSCL, B.P. 108, 59652 Villeneuve d'Ascq, France. Electronic address:

Published: January 2015

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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http://dx.doi.org/10.1016/j.ejmech.2014.11.065DOI Listing

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