Artigo Revisado por pares

Synthesis and in vitro antiplasmodial activity of ferrocenyl aminoquinoline derivatives

2014; Elsevier BV; Volume: 90; Linguagem: Inglês

10.1016/j.ejmech.2014.11.065

ISSN

1768-3254

Autores

Gabin Mwande-Maguene, Jean-Bernard Lékana-Douki, Elisabeth Mouray, Till Bousquet, Philippe Grellier, Sylvain Pellegrini, Fousseyni Samba Toure Ndouo, Jacques Lébibi, Lydie Pélinski,

Tópico(s)

Synthesis and Biological Evaluation

Resumo

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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