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Molecules, Vol. 23, Pages 1453: Anti-Mycobacterium tuberculosis Activity of Esters of Quinoxaline 1,4-Di-N-Oxide

Molecules, Vol. 23, Pages 1453: Anti-Mycobacterium tuberculosis Activity of Esters of Quinoxaline 1,4-Di-N-Oxide

Molecules doi: 10.3390/molecules23061453

Authors: Isidro Palos Julieta Luna-Herrera Edgar E. Lara-Ramírez Alejandra Loera-Piedra Emanuel Fernández-Ramírez Ma. Guadalupe Aguilera-Arreola Alma D. Paz-González Antonio Monge Baojie Wan Scott Franzblau Gildardo Rivera

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.

Authors:   Palos, Isidro ; Luna-Herrera, Julieta ; Lara-Ramírez, Edgar E.; Loera-Piedra, Alejandra ; Fernández-Ramírez, Emanuel ; Aguilera-Arreola, Ma. Guadalupe; Paz-González, Alma D.; Monge, Antonio ; Wan, Baojie ; Franzblau, Scott ; Rivera, Gildardo
Journal:   Molecules
Volume:   23
edition:   6
Year:   2018
Pages:   1453
DOI:   10.3390/molecules23061453
Publication date:   15-Jun-2018
Facts, background information, dossiers
  • Mycobacterium tuberculosis
  • tuberculosis
  • molecules
  • mic
  • drugs
  • drug resistance
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