Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cy...

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Bibliographic Details
Main Authors: Pérez-Silanes, S. (Silvia), Torres, E. (Enrique), Arbillaga, L. (Leire), Varela, J. (Javier), Cerecetto, H. (Hugo), Gonzalez, M. (Mercedes), Azqueta, A. (Amaya), Moreno-de-Viguri, E. (Elsa)
Format: info:eu-repo/semantics/article
Language:eng
Published: Elsevier 2016
Subjects:
Chagas disease
Trypanosoma cruzi
Quinoxaline N-oxide
Cytotoxicity
Genotoxicity
Materias Investigacion::Farmacia::Química farmacéutica
Materias Investigacion::Farmacia::Farmacia y farmacología
Online Access:https://hdl.handle.net/10171/40413
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Summary:Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.

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