Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents

Tapia, RA; Salas, CO; Vazquez, K; Espinosa-Bustos, C; Soto-Delgado, J; Varela, J; Birriel, E; Cerecetto H.; Gonzalez, M.; Paulino M.

Abstract

A new indole-4,9-dione and their phenoxy derivatives were synthesized and evaluated in vitro against the epimastigote form of Trypanosoma cruzi, Y strain. All of these novel compounds were found to be extremely potent and selective that the standard drug nifurtimox. Interestingly, phenoxyindole-4,9-dione 9d displayed excellent nanomolar inhibitory activity, IC50 = 20 nM, and high selectivity index, SI = 625. In silico studies using MOE program were performed to generate a preliminary pharmacophore model. (C) 2014 Elsevier Ltd. All rights reserved.

Más información

Título según WOS: Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents
Título según SCOPUS: Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents
Título de la Revista: BIOORGANIC MEDICINAL CHEMISTRY LETTERS
Volumen: 24
Número: 16
Editorial: PERGAMON-ELSEVIER SCIENCE LTD
Fecha de publicación: 2014
Página de inicio: 3919
Página final: 3922
Idioma: English
DOI:

10.1016/j.bmcl.2014.06.044

Notas: ISI, SCOPUS - ISI