Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
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 deriv...
| Autores: | , , , , , , , , , , , , , , |
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| Tipo de documento: | artigo |
| Data de publicação: | 2013 |
| País: | España |
| Recursos: | Universidad de Navarra |
| Repositório: | Dadun. Depósito Académico Digital de la Universidad de Navarra |
| Idioma: | inglês |
| OAI Identifier: | oai:dadun.unav.edu:10171/35794 |
| Acesso em linha: | https://hdl.handle.net/10171/35794 |
| Access Level: | Acceso aberto |
| Palavra-chave: | Reduction potential Cytotoxicity Mutagenicity Quinoxaline 1,4-di-N-oxide Trypanosoma cruzi Chagas disease |
| Resumo: | 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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