Full metadata record
DC Field | Value | Language |
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dc.creator | Palos, I. (Isidro) | - |
dc.creator | Luna-Herrera, J. (Julieta) | - |
dc.creator | Lara-Ramírez, E. (Edgar E.) | - |
dc.creator | Loera-Piedra, A. (Alejandra) | - |
dc.creator | Fernández-Ramírez, E. (Emanuel) | - |
dc.creator | Aguilera-Arreola, M.G. (Ma. Guadalupe) | - |
dc.creator | Paz-González, A.D. (Alma D.) | - |
dc.creator | Monge, A. (Antonio) | - |
dc.creator | Wan, B. (Baojie) | - |
dc.creator | Franzblau, S.G. (Scott G.) | - |
dc.creator | Rivera, G. (Gildardo) | - |
dc.date.accessioned | 2023-03-01T12:28:24Z | - |
dc.date.available | 2023-03-01T12:28:24Z | - |
dc.date.issued | 2018 | - |
dc.identifier.citation | Palos, I. (Isidro); Luna-Herrera, J. (Julieta); Lara-Ramírez, E. (Edgar E.); et al. "Anti-mycobacterium tuberculosis activity of esters of quinoxaline 1,4-Di-N-Oxide". Molecules. 23 (6), 2018, 1453 | es |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | https://hdl.handle.net/10171/65595 | - |
dc.description.abstract | Tuberculosis 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 |
dc.description.sponsorship | : This research was funded by Secretaria de Investigación y Posgrado-Instituto Politécnico Nacional, grant number (G.R.: SIP-SIP-20170207 and SIP-20180306; J.L.-H.: 20170126 and 20180411; and M.G.A.-A.: 20170230 and 20180324). | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | MDPI AG | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.subject | Esters | es_ES |
dc.subject | Quinoxaline 1,4-di-N-oxide | es_ES |
dc.subject | Mycobacterium tuberculosis | es_ES |
dc.subject | DNA gyrase | es_ES |
dc.subject | Drug resistance | es_ES |
dc.title | Anti-mycobacterium tuberculosis activity of esters of quinoxaline 1,4-Di-N-Oxide | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.description.note | This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). | es_ES |
dc.identifier.doi | 10.3390/molecules23061453 | - |
dadun.citation.number | 6 | es_ES |
dadun.citation.publicationName | Molecules | es_ES |
dadun.citation.startingPage | 1453 | es_ES |
dadun.citation.volume | 23 | es_ES |
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