Anti-Mycobacterium tuberculosis Activity of Esters of Quinoxaline 1,4-Di-N-Oxide

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AudienciaPúblico en generales_ES
CoberturaMéxicoes_ES
Fecha de ingreso2026-09-15T00:30:14Z
Fecha de publicación2018-01-01
ResumenTuberculosis continues to be a public health problem in the world, and drug resistance has been a major obstacle in its treatment. Quinoxaline 1,4-di-N-oxide has been proposed as a scaffold to design new drugs to combat this disease. To examine the efficacy of this compound, this study evaluates methyl, ethyl, isopropyl, and n-propyl esters of quinoxaline 1,4-di-N-oxide derivatives in vitro against Mycobacterium tuberculosis (pansusceptible and monoresistant strains). Additionally, the inhibitory effect of esters of quinoxaline 1,4-di-N-oxide on M. tuberculosis gyrase supercoiling was examined, and a stability analysis by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS) was also carried out. Results showed that eight compounds (T-007, T-018, T-011, T-069, T-070, T-072, T-085 and T-088) had an activity similar to that of the reference drug isoniazid (minimum inhibitory concentration (MIC) = 0.12 µg/mL) with an effect on nonreplicative cells and drug monoresistant strains. Structural activity relationship analysis showed that the steric effect of an ester group at 7-position is key to enhancing its biological effects. Additionally, T-069 showed a high stability after 24 h in human plasma at 37 °C.es_ES
Doihttps://doi.org/10.3390/molecules23061453es_ES
URIhttps://riuat.uat.edu.mx/handle/123456789/2173
Idiomaeses_ES
EditorialMDPI AGes_ES
RelaciónMoleculeses_ES
URL relacionadohttps://doi.org/10.3390/molecules23061453es_ES
DerechosAcceso abierto (Metadatos de producción científica)es_ES
Licenciahttp://purl.org/coar/access_right/c_abf2es_ES
FuenteMolecules
TítuloAnti-Mycobacterium tuberculosis Activity of Esters of Quinoxaline 1,4-Di-N-Oxidees_ES
TipoArtículoes_ES
ArbitradoHa sido Arbitradoes_ES
AutorPalos, Isidro
AutorLuna-Herrera, Julieta
AutorLara-Ramírez, Edgar E.
AutorLoera-Piedra, Alejandra
AutorFernández-Ramírez, Emanuel
AutorAguilera-Arreola, Ma. Guadalupe
AutorPaz-González, Alma D.
AutorMonge, Antonio
AutorWan, Baojie
AutorFranzblau, Scott
AutorRivera, Gildardo
AutorPalos, Isidroes_ES
AutorLuna-Herrera, Julietaes_ES
AutorLara-Ramírez, Edgar E.es_ES
AutorLoera-Piedra, Alejandraes_ES
AutorFernández-Ramírez, Emanueles_ES
AutorAguilera-Arreola, Ma. Guadalupees_ES
AutorPaz-González, Alma D.es_ES
AutorMonge, Antonioes_ES
AutorWan, Baojiees_ES
AutorFranzblau, Scottes_ES
AutorRivera, Gildardoes_ES
InstituciónUniversidad Autónoma de Tamaulipas
InstituciónUniversidad Autónoma de Tamaulipases_ES
Número6es_ES
Rango de páginas1453es_ES
URL relacionadahttps://doi.org/10.3390/molecules23061453
Tipo de artículoIndexado
Tipo de artículoIndexadoes_ES
Volumen23es_ES

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