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Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di- N -oxide derivatives as potential antitubercular agents.

Alonzo Gonzalez-GonzalezOscar Sánchez-SánchezBaojie WanScott G FranzblauIsidro PalosJosé Carlos Espinoza-HicksAdriana Moreno-RodríguezAna Verónica Martínez-VázquezEdgar E Lara-RamírezEyra Ortiz-PérezAlma D Paz-GonzálezGildardo Rivera
Published in: RSC medicinal chemistry (2024)
Tuberculosis is a worldwide health problem that warrants attention given that the current treatment options require a long-term chemotherapeutic period and have reported the development of Mycobacterium tuberculosis ( M. tuberculosis ) multidrug resistant strains. In this study, n -butyl and isobutyl quinoxaline-7-carboxylate 1,4-di- N -oxide were evaluated against replicating and non-replicating H37Rv M. tuberculosis strains. The results showed that seventeen of the twenty-eight derivatives have minimum inhibitory concentration (MIC) values lower than isoniazid (2.92 μM). The most active antimycobacterial agents were T-148 , T-149 , T-163 , and T-164 , which have the lowest MIC values (0.53, 0.57, 0.53, and 0.55 μM respectively). These results confirm the potential of quinoxaline-1,4-di- N -oxide against M. tuberculosis to develop and obtain new and more safety antituberculosis drugs.
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