ARTÍCULO

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

Autores: Torres Pastor, Enrique; Moreno de Viguri, Elsa; Galiano Ruiz, Silvia; G. Devarapally; P. W. Crawford; Azqueta Oscoz, Amaya; Arbillaga Lacunza, Leire; J. Varela; E. Birriel; R. Di Maio; H. Cerecetto; M. González; Aldana Moraza, Ignacio; Monge Vega, Antonio; Pérez Silanes, Silvia
Título de la revista: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN: 0223-5234
Volumen: 66
Páginas: 324 - 334
Fecha de publicación: 2013
Resumen:
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-N-oxide 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.