Anti-Trypanosoma cruzi and anti-leishmanial activity by quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives

Juan Carlos Villalobos-Rocha, Luvia Sánchez-Torres, Benjamín Nogueda-Torres, Aldo Segura-Cabrera, Carlos A. García-Pérez, Virgilio Bocanegra-García, Isidro Palos, Antonio Monge, Gildardo Rivera

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26 Scopus citations

Abstract

In this work, a novel series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives were evaluated in vitro on Trypanosoma cruzi trypomastigotes and Leishmania mexicana promastigotes, and cytotoxicity activity in murine macrophages was tested. In silico molecular docking simulations of trypanothione reductase were also done. Three compounds of 33 quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives showed better anti-T. cruzi activity than nifurtimox and beznidazole; two compounds had better anti-leishmanial activity that amphotericin-B, and two compounds showed better activity against both parasites than reference drugs. Compounds M2, M7, M8 and E5, showed low cytotoxic activity on the host cell. The in silico studies suggest that compound M2 is a potential trypanothione reductase inhibitor. © 2014 Springer-Verlag.
Original languageAmerican English
Pages (from-to)2027-2035
Number of pages1823
JournalParasitology Research
DOIs
StatePublished - 1 Jan 2014

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