Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery

Design, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine compounds with promising in vitro (55, 56, 61, 64, 66, and 70–73) and in v...

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Published in:European journal of medicinal chemistry 2018-05, Vol.152, p.489-514
Main Authors: Quiliano, Miguel, Pabón, Adriana, Moles, Ernest, Bonilla-Ramirez, Leonardo, Fabing, Isabelle, Fong, Kim Y., Nieto-Aco, Diego A., Wright, David W., Pizarro, Juan C., Vettorazzi, Ariane, López de Cerain, Adela, Deharo, Eric, Fernández-Busquets, Xavier, Garavito, Giovanny, Aldana, Ignacio, Galiano, Silvia
Format: Article
Language:English
Subjects:
Antimalarial
Antiplasmodial
Arylamino alcohol
Chemical Sciences
Enantiomer separation
Hsp90
Multi-stage activity
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Summary:Design, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine compounds with promising in vitro (55, 56, 61, 64, 66, and 70–73) and in vivo (66 and 72) antimalarial profiles against Plasmodium falciparum and Plasmodium berghei. Compounds 55, 56, 61, 64, 66 and 70–73 exhibited potent antiplasmodial activity against chloroquine-resistant strain FCR-3 (IC50s 
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2018.04.038