In vitro and in silico evaluations of new aryloxy-1,4-naphthoquinones as anti-Trypanosoma cruzi agents

Alejandra González, Nohemí Becerra, Muhammad Kashif, Mercedes González, Hugo Cerecetto, Elena Aguilera, Benjamín Nogueda-Torres, Karla F. Chacón-Vargas, J. José Zarate-Ramos, Uziel Castillo-Velázquez, Cristian O. Salas, Gildardo Rivera, Karina Vázquez

Resultado de la investigación: Contribución a una revistaArtículorevisión exhaustiva

4 Citas (Scopus)

Resumen

© 2020, Springer Science+Business Media, LLC, part of Springer Nature. In the search for new therapeutic alternatives for Chagas disease, a series of six aryloxy -naphthoquinone derivatives were synthesized and evaluated in vitro against Trypanosoma cruzi epimastigotes of the Tulahuén 2, INC-5, and NINOA strains. The compounds 3d and 4a showed better or similar trypanosomicidal activity than the reference drug nifurtimox. In addition, 3d and 4a also elicited better trypanosomicidal activity than nifurtimox against T. cruzi bloodstream trypomastigotes. On the other hand, 3b showed the highest selective indexes (SI values between 44 and 500, in the three T. cruzi strains). Finally, molecular docking studies suggested that these compounds could be potential trypanothione reductase inhibitors. Therefore, based on these new results, we validated that the aryloxy-naphthoquinone scaffold is essential to obtain more selective cytotoxic and trypanosomicidal compounds.
Idioma originalInglés estadounidense
Páginas (desde-hasta)665-674
Número de páginas10
PublicaciónMedicinal Chemistry Research
DOI
EstadoPublicada - 1 abr 2020

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