1. Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
- Author
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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), and Torres, E. (Enrique)
- Subjects
Chagas disease ,Reduction potential ,Mutagenicity ,Cytotoxicity ,Trypanosoma cruzi ,Quinoxaline 1,4-di-N-oxide - 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
- Published
- 2013