Some quinoline-based compounds bearing a ferrocenyl unit in the 2-position of the heterocyclic system were synthesized from ferrocenyl-o-nitrochalcones through a simple hydrogenation/intramolecular cyclization sequence and fully characterized. The obtained ferrocenyl derivatives were evaluated in vitro as antimalarial agents against chloroquine-susceptible D10 and chloroquine-resistant W2 strains of Plasmodium falciparum and a beneficial effect of the organometallic moiety was evidenced in comparison with the phenyl-substituted analogues. All the ferrocenyl heterocycles inhibited the parasite growth in ?M range and the lowest values of IC50 were determined for derivatives containing a dimethylamino group as additional substituent.

Synthesis of 2-ferrocenylquinoline derivatives and evaluation of their antimalarial activity

Patti Angela;Pedotti Sonia;
2012

Abstract

Some quinoline-based compounds bearing a ferrocenyl unit in the 2-position of the heterocyclic system were synthesized from ferrocenyl-o-nitrochalcones through a simple hydrogenation/intramolecular cyclization sequence and fully characterized. The obtained ferrocenyl derivatives were evaluated in vitro as antimalarial agents against chloroquine-susceptible D10 and chloroquine-resistant W2 strains of Plasmodium falciparum and a beneficial effect of the organometallic moiety was evidenced in comparison with the phenyl-substituted analogues. All the ferrocenyl heterocycles inhibited the parasite growth in ?M range and the lowest values of IC50 were determined for derivatives containing a dimethylamino group as additional substituent.
2012
Istituto di Chimica Biomolecolare - ICB - Sede Pozzuoli
Ferrocenyl chalcones; Hydrogenation/intramolecular cyclization sequence;Quinoline-based ferrocenes; Bioactive organometallics; Antimalarial assay
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/241334
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