TY - JOUR
T1 - Anti-Trypanosoma cruzi and anti-leishmanial activity by quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives
AU - Villalobos-Rocha, Juan Carlos
AU - Sánchez-Torres, Luvia
AU - Nogueda-Torres, Benjamín
AU - Segura-Cabrera, Aldo
AU - García-Pérez, Carlos A.
AU - Bocanegra-García, Virgilio
AU - Palos, Isidro
AU - Monge, Antonio
AU - Rivera, Gildardo
N1 - Funding Information:
Acknowledgments Juan Carlos Villalobos-Rocha is the recipient of a scholarship (228946) from CONACyT, Mexico. Benjamin Nogueda-Torres, Luvia Sánchez-Torres, Virgilio Bocanegra-García, and Gildardo Rivera hold a scholarship from the Comisión de Operación y Fomento de Actividades Académicas (COFAA-Instituto Politécnico Nacional) and the Programa de Estímulos al Desempeño de los Investigadores (EDI-Instituto Politécnico Nacional). Our gratitude to Lilia C. Gómez-Caro, Mario Sánchez-Sánchez, and Jesus Villegas-Mendoza for their support in this project. We wish to express our gratitude to the CONACyT (CB-2010-01, clave 0157358) and the Secretaria de Investigación y Posgrado of Instituto Politecnico Nacional (SIP-20130637 and SIP-20130768) for their financial support of this study.
PY - 2014/6
Y1 - 2014/6
N2 - 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.
AB - 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.
KW - Biological activity
KW - Leishmania mexicana
KW - Molecular docking
KW - Quinoxaline 1,4-di-N-oxide
KW - Trypanosoma cruzi
KW - Trypanothione reductase
UR - http://www.scopus.com/inward/record.url?scp=84903816590&partnerID=8YFLogxK
U2 - 10.1007/s00436-014-3850-8
DO - 10.1007/s00436-014-3850-8
M3 - Artículo
C2 - 24691716
SN - 0932-0113
VL - 113
SP - 2027
EP - 2035
JO - Parasitology Research
JF - Parasitology Research
IS - 6
ER -