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In vitro and in silico analysis of new n-butyl and isobutyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives against trypanosoma cruzi as Trypanothione reductase inhibitors

American trypanosomiasis is a worldwide health problem that requires attention due to ineffective treatment options. We evaluated n-butyl and isobutyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives against trypomastigotes of the Trypanosoma cruzi strains NINOA and INC-5. An in silico analysis...

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Hauptverfasser: González-González, Alonzo (VerfasserIn) , Sánchez-Sánchez, Oscar (VerfasserIn) , Krauth-Siegel, Renate (VerfasserIn) , Bolognesi, Maria Laura (VerfasserIn) , Gớmez-Escobedo, Rogelio (VerfasserIn) , Nogueda-Torres, Benjamín (VerfasserIn) , Vázquez-Jiménez, Lenci K. (VerfasserIn) , Saavedra, Emma (VerfasserIn) , Encalada, Rusely (VerfasserIn) , Espinoza-Hicks, José Carlos (VerfasserIn) , Paz-González, Alma D. (VerfasserIn) , Rivera, Gildardo (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 1 November 2022
In: International journal of molecular sciences
Year: 2022, Jahrgang: 23, Heft: 21, Pages: 1-18
ISSN:1422-0067
DOI:10.3390/ijms232113315
Online-Zugang:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.3390/ijms232113315
Verlag, lizenzpflichtig, Volltext: https://www.mdpi.com/1422-0067/23/21/13315
Volltext
Verfasserangaben:Alonzo González-González, Oscar Sánchez-Sánchez, R. Luise Krauth-Siegel, Maria Laura Bolognesi, Rogelio Gớmez-Escobedo, Benjamín Nogueda-Torres, Lenci K. Vázquez-Jiménez, Emma Saavedra, Rusely Encalada, José Carlos Espinoza-Hicks, Alma D. Paz-González and Gildardo Rivera
Beschreibung
Zusammenfassung:American trypanosomiasis is a worldwide health problem that requires attention due to ineffective treatment options. We evaluated n-butyl and isobutyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives against trypomastigotes of the Trypanosoma cruzi strains NINOA and INC-5. An in silico analysis of the interactions of 1,4-di-N-oxide on the active site of trypanothione reductase (TR) and an enzyme inhibition study was carried out. The n-butyl series compound identified as T-150 had the best trypanocidal activity against T. cruzi trypomastigotes, with a 13% TR inhibition at 44 μM. The derivative T-147 behaved as a mixed inhibitor with Ki and Ki’ inhibition constants of 11.4 and 60.8 µM, respectively. This finding is comparable to the TR inhibitor mepacrine (Ki = 19 µM).
Beschreibung:Gesehen am 20.01.2023
Beschreibung:Online Resource
ISSN:1422-0067
DOI:10.3390/ijms232113315

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