In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents

In this study, a series of 22 pre-synthesized 7-chloro-4-mino(oxy)quinoline derivatives was assayed in vitro as potential antichagasic agents. A primary screening against Trypanosoma cruzi epimastigotes and a non-specific cytotoxicity assay on murine fibroblasts were simultaneously performed, resulting quinolines 3, 7 and 12 with great selectivity (SI) on the extracellular parasite (SI7, SI3 , SI12 and SIBZ >9.44). Therefore, the activity of these derivatives was evaluated on intracellular amastigotes, achieving derivative 7 the best SI (SI = 12.73). These results, supported by the in silico prediction of a good oral bioavailability and a suitable risk profile, propose the 4-amino-7-chloroquinoline scaffold as a potential template for designing trypanocidal prototypes.

• Fecha de publicación: 2014
• Institución: Ministerio de Ciencia, Tecnología e Innovación
• Repositorio: Repositorio Minciencias
• Idioma: eng
• OAI Identifier: oai:repositorio.minciencias.gov.co:20.500.14143/34179
• Acceso en línea: http://repositorio.colciencias.gov.co/handle/11146/34179
• Palabra clave: Biología vegetal; Productos químicos; Trypanosoma cruzi; Chloroquinoline derivatives; Cytotoxicity Lipinski’s rule; OSIRIS software; Aceites esenciales; Biotecnología; Tecnología química; Biomasa; Biología vegetal; Biomasa
• License: http://purl.org/coar/access_right/c_f1cf