2019-04-012019-04-0120140960-894Xhttp://repositorio.colciencias.gov.co/handle/11146/34179In 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.pdf5 páginasenginfo:eu-repo/semantics/embargoedAccessIn vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agentsArtículo científicoContiene 53 referencias bibliográficas. Véase documento adjunto10.1016/j.bmcl.2013.12.071Biología vegetalProductos químicosTrypanosoma cruziChloroquinoline derivativesCytotoxicity Lipinski’s ruleOSIRIS softwareAceites esencialesBiotecnologíaTecnología químicaBiomasaBiología vegetalBiomasa