Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
Keywords: 
Reduction potential
Cytotoxicity
Mutagenicity
Quinoxaline 1,4-di-N-oxide
Trypanosoma cruzi
Chagas disease
Issue Date: 
30-May-2013
Publisher: 
Elsevier
ISSN: 
0223-5234
Citation: 
Torres E, Moreno-Viguri E, Galiano S, Devarapally G, Crawford PW, Azqueta A, et al. Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents. Eur J Med Chem 2013 8;66(0):324-334
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

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