Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytot...

Descripción completa

Detalles Bibliográficos
Autores: Pérez-Silanes, S. (Silvia)|||/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45, Torres, E. (Enrique)|||/items/63f6c247-849f-4192-9a16-b86398ba3fc5, Arbillaga, L. (Leire)|||/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39, Varela, J. (Javier)|||/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24, Cerecetto, H. (Hugo)|||/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c, Gonzalez, M. (Mercedes)|||/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554, Azqueta, A. (Amaya)|||/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893, Moreno-de-Viguri, E. (Elsa)|||/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa
Tipo de recurso: artículo
Fecha de publicación:2016
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/40413
Acceso en línea:https://hdl.handle.net/10171/40413
Access Level:acceso abierto
Palabra clave:Chagas disease
Trypanosoma cruzi
Quinoxaline N-oxide
Cytotoxicity
Genotoxicity
Materias Investigacion::Farmacia::Química farmacéutica
Materias Investigacion::Farmacia::Farmacia y farmacología
Descripción
Sumario:Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.