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

Pérez-Silanes, S. (Silvia); Torres, E. (Enrique); Arbillaga, L. (Leire); Varela, J. (Javier); Cerecetto, H. (Hugo); Gonzalez, M. (Mercedes); Azqueta, A. (Amaya); Moreno-de-Viguri, E. (Elsa)

Authors:

Pérez-Silanes, S. (Silvia)

Torres, E. (Enrique)

Arbillaga, L. (Leire)

Varela, J. (Javier)

Cerecetto, H. (Hugo)

Gonzalez, M. (Mercedes)

Azqueta, A. (Amaya)

Moreno-de-Viguri, E. (Elsa)

Keywords:

Chagas disease
Trypanosoma cruzi
Quinoxaline N-oxide
Cytotoxicity
Genotoxicity
Materias Investigacion::Farmacia::Química farmacéutica
Materias Investigacion::Farmacia::Farmacia y farmacología

Issue Date:

2016

Publisher:

Elsevier

ISSN:

0960-894X

Citation:

Pérez-Silanes S, Torres E, Arbillaga L, Varela J, Cerecetto H, González M, et al. Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity. Bioorg Med Chem Lett 2016;26(3):903–906

Abstract

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.

URI:

https://hdl.handle.net/10171/40413

DOI:

http://dx.doi.org/10.1016/j.bmcl.2015.12.070

Appears in Collections:

DA - Farmacia - Farmacología - Artículos de revista
DA - Farmacia - Orgánica - Artículos de revista
DA - Instituto de Salud Tropical - Artículos de revista

Files in This Item: