| dc.creator | Kouznetsov, Vladimir V. | |
| dc.creator | Gómez Barrio, Alicia | |
| dc.creator | Escario, José A. | |
| dc.creator | Rojas Ruiz, Fernando A. | |
| dc.creator | Fonseca Berzal, Cristina | |
| dc.date | 2019-04-01T03:39:59Z | |
| dc.date | 2019-04-01T03:39:59Z | |
| dc.date | 2014 | |
| dc.date | info:eu-repo/date/embargoEnd/2024-01-31 | |
| dc.date.accessioned | 2022-12-07T13:30:46Z | |
| dc.date.available | 2022-12-07T13:30:46Z | |
| dc.identifier | 0960-894X | |
| dc.identifier | http://repositorio.colciencias.gov.co/handle/11146/34179 | |
| dc.identifier | Contiene 53 referencias bibliográficas. Véase documento adjunto | |
| dc.identifier | 10.1016/j.bmcl.2013.12.071 | |
| dc.identifier.uri | https://repositorioslatinoamericanos.uchile.cl/handle/2250/5298076 | |
| dc.description | 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. | |
| dc.description | Departamento Administrativo de Ciencia, Tecnología e Innovación [CO] Colciencias | |
| dc.description | 5507-543-31904 | |
| dc.description | Programa: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana | |
| dc.description | no | |
| dc.format | pdf | |
| dc.format | 5 páginas | |
| dc.format | application/pdf | |
| dc.language | eng | |
| dc.relation | Programa: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana. La publicación completa está disponible en : <a href="http://repositorio.colciencias.gov.co/handle/11146/34163" target="blank">http://repositorio.colciencias.gov.co/handle/11146/34163</a> | |
| dc.rights | info:eu-repo/semantics/embargoedAccess | |
| dc.source | Bioorganic & Medicinal Chemistry Letters 24 (2014) 1209-1213 | |
| dc.subject | Biología vegetal | |
| dc.subject | Productos químicos | |
| dc.subject | Trypanosoma cruzi | |
| dc.subject | Chloroquinoline derivatives | |
| dc.subject | Cytotoxicity Lipinski’s rule | |
| dc.subject | OSIRIS software | |
| dc.subject | Aceites esenciales | |
| dc.subject | Biotecnología | |
| dc.subject | Tecnología química | |
| dc.subject | Biomasa | |
| dc.subject | Biología vegetal | |
| dc.subject | Biomasa | |
| dc.title | In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents | |
| dc.type | info:eu-repo/semantics/article | |
| dc.type | info:eu-repo/semantics/publishedVersion | |
| dc.coverage | Colombia | |
