Lara-Ramírez, E. (Edgar E.)

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    Anti-mycobacterium tuberculosis activity of esters of quinoxaline 1,4-Di-N-Oxide
    (MDPI AG, 2018) Aguilera-Arreola, M.G. (Ma. Guadalupe); Wan, B. (Baojie); Franzblau, S.G. (Scott G.); Lara-Ramírez, E. (Edgar E.); Palos, I. (Isidro); Loera-Piedra, A. (Alejandra); Rivera, G. (Gildardo); Monge, A. (Antonio); Paz-González, A.D. (Alma D.); Fernández-Ramírez, E. (Emanuel); Luna-Herrera, J. (Julieta)
    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.