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Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents

Authors :
Pérez-Silanes, S. (Silvia)
Monge, A. (Antonio)
Aldana, I. (Ignacio)
Gonzalez, M. (Mercedes)
Cerecetto, H. (Hugo)
Di-Maio, R. (Rossanna)
Birriel, E. (Estefanía)
Varela, J. (Javier)
Arbillaga, L. (Leire)
Azqueta, A. (Amaya)
Crawford, P.W. (Philip W.)
Devarapally, G. (Goutham)
Galiano, S. (Silvia)
Moreno-de-Viguri, E. (Elsa)
Torres, E. (Enrique)
Source :
Dadun. Depósito Académico Digital de la Universidad de Navarra, instname
Publication Year :
2013
Publisher :
Elsevier, 2013.

Abstract

As a continuation of our research and with the aim of obtaining new agents against Chagas disease, an extremely neglected disease which threatens 100 million people, eighteen new quinoxaline 1,4-di-Noxide derivatives have been synthesized following the Beirut reaction. The synthesis of the new derivatives was optimized through the use of a new and more efficient microwave-assisted organic synthetic method. The new derivatives showed excellent in vitro biological activity against Trypanosoma cruzi. Compound 17, which was substituted with fluoro groups at the 6- and 7-positions of the quinoxaline ring, was the most active and selective in the cytotoxicity assay. The electrochemical study showed that the most active compounds, which were substituted by electron-withdrawing groups,possessed a greater ease of reduction of the N-oxide groups

Details

Database :
OpenAIRE
Journal :
Dadun. Depósito Académico Digital de la Universidad de Navarra, instname
Accession number :
edsair.dedup.wf.001..9c7ec55de3d55f90933ab61c796770cb