1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawin...

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Detalles Bibliográficos
Autores principales: Kumar, Kewal, Pradines, Bruno, Madamet, Marilyn, Amalvict, Rémy, Benoit, Nicolas, Kumar, Vipan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126053/
https://www.ncbi.nlm.nih.gov/pubmed/25440881
http://dx.doi.org/10.1016/j.ejmech.2014.10.024
Descripción
Sumario:1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC(50) values of 3.76 and 4.58 μM against 3D7 and W2 strains, respectively.

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