Biological Evaluation of Esters of 4-Carboxylate-1,2,3-triazine and Analogs as New Potential Anti-Mycobacterium tuberculosis Agents

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AudienciaPúblico en generales_ES
CoberturaMéxicoes_ES
Fecha de ingreso2026-09-15T00:30:14Z
Fecha de publicación2026-01-01
ResumenIn searching for novel molecules to act as antibacterial agents, particularly against Mycobacterium tuberculosis bacteria, three series of C5- and C6-substituted 1,2,3-triazine compounds were investigated: 1,2,3-triazine-4-carboxylate 1-oxide (series 1), 1,2,3-triazine-4-carboxylate (series 2), and 3,6-dihydro-1,2,3-triazine-4-carboxylate 1-oxide derivatives (series 3). Their structural elucidation was confirmed by 1H-NMR, 13C-NMR, and HRMS. We determined their antibacterial activity (MIC value) using the MABA against the M. tuberculosis H37Rv strain, as well as their physicochemical and pharmacokinetic properties. Finally, to determine their potential mode of action, an inhibition assay against M. tuberculosis DNA gyrase was performed. Compounds 4-ethoxycarbonyl-5-(3-methoxyphenyl)-1,2,3-triazine (2l) and 4-ethoxycarbonyl-5 -(n-propyl)-1,2,3-triazine (3s) exhibited high activity against M. tuberculosis with MIC values < 5.90 µg/mL and selectivity index of 18.56 and 8.36, respectively. Additionally, compound 2m also exhibited anti-mycobacterial activity with MIC values < 10.0 µg/mL. However, none of the selected compounds inhibited the activity of M. tuberculosis DNA gyrase, suggesting that another drug target may be involved as a mode of action. These results encourage exploring the use of 1,2,3-triazine as a scaffold for the development of new anti-mycobacterium agents.es_ES
Doihttps://doi.org/10.3390/molecules31121993es_ES
URIhttps://riuat.uat.edu.mx/handle/123456789/2175
Idiomaeses_ES
EditorialMDPI AGes_ES
RelaciónMoleculeses_ES
URL relacionadohttps://doi.org/10.3390/molecules31121993es_ES
DerechosAcceso abierto (Metadatos de producción científica)es_ES
Licenciahttp://purl.org/coar/access_right/c_abf2es_ES
FuenteMolecules
TítuloBiological Evaluation of Esters of 4-Carboxylate-1,2,3-triazine and Analogs as New Potential Anti-Mycobacterium tuberculosis Agentses_ES
TipoArtículoes_ES
ArbitradoHa sido Arbitradoes_ES
AutorRivera, Gildardo
AutorNavarrete-Carriola, Diana V.
AutorAngelis, Luca De
AutorPaz-González, Alma D.
AutorMartínez-Vázquez, Ana Verónica
AutorOrtiz-Pérez, Eyra
AutorWan, Baojie
AutorFranzblau, Scott
AutorMartínez-Archundia, Marlet
AutorMoreno-Rodríguez, Adriana
AutorPalos, Isidro
AutorDoyle, Michael P.
AutorRivera, Gildardoes_ES
AutorNavarrete-Carriola, Diana V.es_ES
AutorAngelis, Luca Dees_ES
AutorPaz-González, Alma D.es_ES
AutorMartínez-Vázquez, Ana Verónicaes_ES
AutorOrtiz-Pérez, Eyraes_ES
AutorWan, Baojiees_ES
AutorFranzblau, Scottes_ES
AutorMartínez-Archundia, Marletes_ES
AutorMoreno-Rodríguez, Adrianaes_ES
AutorPalos, Isidroes_ES
AutorDoyle, Michael P.es_ES
InstituciónUniversidad Autónoma de Tamaulipas
InstituciónUniversidad Autónoma de Tamaulipases_ES
Número12es_ES
Rango de páginas1993es_ES
URL relacionadahttps://doi.org/10.3390/molecules31121993
Tipo de artículoIndexado
Tipo de artículoIndexadoes_ES
Volumen31es_ES

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