Artículos de revista (Inst. Salud Tropical)
Permanent URI for this collectionhttps://hdl.handle.net/10171/52056
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- Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents(Elsevier, 2013-05-30) Devarapally, G. (Goutham); Aldana, I. (Ignacio); Torres, E. (Enrique); Gonzalez, M. (Mercedes); Varela, J. (Javier); Di-Maio, R. (Rossanna); Birriel, E. (Estefanía); Arbillaga, L. (Leire); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Moreno-de-Viguri, E. (Elsa); Cerecetto, H. (Hugo); Azqueta, A. (Amaya); Crawford, P.W. (Philip W.)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