Esters of quinoxaline-7-carboxylate-1,4-di- N -oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors
| Audiencia | Público en general | es_ES |
| Cobertura | México | es_ES |
| Fecha de ingreso | 2026-09-15T00:30:13Z | |
| Fecha de publicación | 2020-01-01 | |
| Resumen | Abstract Trichomoniasis is a public health problem worldwide. Trichomoniasis treatment consists of the use of nitroimidazole derivatives; however, therapeutic ineffectiveness occurs in 5 to 20 % of the cases. Therefore, it is essential to propose new pharmacological agents against this disease. In this work, esters of quinoxaline-7-carboxylate-1,4-di- N -oxide (EQX- N O) were evaluated in in vitro assays as novel trichomonicidal agents. Additionally, an in vitro enzyme assay and molecular docking analysis against triosephosphate isomerase of Trichomonas vaginalis to confirm their mechanism of action were performed. Ethyl (compound 12 ) and n -propyl (compound 37 ) esters of quinoxaline-7-carboxy-late-1,4-di- N -oxide derivatives showed trichomonicidal activity comparable to nitazoxanide, whereas five methyl (compounds 5 , 15 , 19 , 20 and 22 ), four isopropyl (compounds 28 , 29 , 30 and 34 ), three ethyl (compounds 4 , 13 and 23 ) and one n propyl (compound 35 ) ester derivatives displayed activity comparable to albendazole. Compounds 6 and 20 decreased 100 % of the enzyme activity of recombinant protein triosephosphate isomerase. | es_ES |
| Doi | https://doi.org/10.2478/acph-2021-0032 | es_ES |
| URI | https://riuat.uat.edu.mx/handle/123456789/2169 | |
| Idioma | es | es_ES |
| Editorial | Walter de Gruyter GmbH | es_ES |
| Relación | Acta Pharmaceutica | es_ES |
| URL relacionado | https://doi.org/10.2478/acph-2021-0032 | es_ES |
| Derechos | Acceso abierto (PDF local verificado) | es_ES |
| Licencia | http://purl.org/coar/access_right/c_abf2 | es_ES |
| Fuente | Acta Pharmaceutica | |
| Título | Esters of quinoxaline-7-carboxylate-1,4-di- N -oxide as Trichomonas vaginalis triosephosphate isomerase inhibitors | es_ES |
| Tipo | Artículo | es_ES |
| Arbitrado | Ha sido Arbitrado | es_ES |
| Autor | Palos, Isidro | |
| Autor | Moo-Puc, Rosa | |
| Autor | Vique-Sánchez, José Luis | |
| Autor | Benítez-Cardoza, Claudia G. | |
| Autor | Monge, Antonio | |
| Autor | Villalobos-Rocha, Juan Carlos | |
| Autor | Paz-Gonzalez, Alma D. | |
| Autor | Rivera, Gildardo | |
| Autor | Palos, Isidro | es_ES |
| Autor | Moo-Puc, Rosa | es_ES |
| Autor | Vique-Sánchez, José Luis | es_ES |
| Autor | Benítez-Cardoza, Claudia G. | es_ES |
| Autor | Monge, Antonio | es_ES |
| Autor | Villalobos-Rocha, Juan Carlos | es_ES |
| Autor | Paz-Gonzalez, Alma D. | es_ES |
| Autor | Rivera, Gildardo | es_ES |
| Institución | Universidad Autónoma de Tamaulipas | |
| Institución | Universidad Autónoma de Tamaulipas | es_ES |
| Número | 3 | es_ES |
| Rango de páginas | 485-495 | es_ES |
| URL relacionada | https://doi.org/10.2478/acph-2021-0032 | |
| Tipo de artículo | Indexado | |
| Tipo de artículo | Indexado | es_ES |
| Volumen | 71 | es_ES |