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| Verfasst von: | González-González, Alonzo [VerfasserIn]  |
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| | Sánchez-Sánchez, Oscar [VerfasserIn] |
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| | Krauth-Siegel, Renate [VerfasserIn] |
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| | Bolognesi, Maria Laura [VerfasserIn] |
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| | Gớmez-Escobedo, Rogelio [VerfasserIn] |
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| | Nogueda-Torres, Benjamín [VerfasserIn] |
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| | Vázquez-Jiménez, Lenci K. [VerfasserIn] |
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| | Saavedra, Emma [VerfasserIn] |
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| | Encalada, Rusely [VerfasserIn] |
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| | Espinoza-Hicks, José Carlos [VerfasserIn] |
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| | Paz-González, Alma D. [VerfasserIn] |
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| | Rivera, Gildardo [VerfasserIn] |
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| Titel: | 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 |
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| Verf.angabe: | 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 |
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| E-Jahr: | 2022 |
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| Jahr: | 1 November 2022 |
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| Umfang: | 18 S. |
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| Fussnoten: | Gesehen am 20.01.2023 |
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| Titel Quelle: | Enthalten in: International journal of molecular sciences |
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| Ort Quelle: | Basel : Molecular Diversity Preservation International, 2000 |
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| Jahr Quelle: | 2022 |
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| Band/Heft Quelle: | 23(2022), 21, Artikel-ID 13315, Seite 1-18 |
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| ISSN Quelle: | 1422-0067 |
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| | 1661-6596 |
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| Abstract: | 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). |
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| DOI: | doi:10.3390/ijms232113315 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.3390/ijms232113315 |
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| | Volltext: https://www.mdpi.com/1422-0067/23/21/13315 |
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| | DOI: https://doi.org/10.3390/ijms232113315 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | 4-di-<i>N</i>-oxide |
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| | Chagas disease |
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| | chemical synthesis |
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| | quinoxaline-1 |
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| | trypanothione reductase |
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| | trypomastigotes |
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| K10plus-PPN: | 1831602482 |
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| Verknüpfungen: | → Zeitschrift |
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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 / González-González, Alonzo [VerfasserIn]; 1 November 2022 (Online-Ressource)
