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

被引:0
|
作者
Gonzalez-Gonzalez, Alonzo [1 ]
Sanchez-Sanchez, Oscar [1 ]
Wan, Baojie [2 ]
Franzblau, Scott [2 ]
Palos, Isidro [3 ]
Espinoza-Hicks, Jose C. [4 ]
Moreno-Rodriguez, Adriana [5 ]
Martinez-Vazquez, Ana Veronica [1 ]
Lara-Ramirez, Edgar E. [1 ]
Ortiz-Perez, Eyra [1 ]
Paz-Gonzalez, Alma D. [1 ]
Rivera, Gildardo [1 ]
机构
[1] Inst Politecn Nacl, Lab Biotecnol Farmaceut, Ctr Biotecnol Genom, Reynosa, Mexico
[2] Univ Illinois, Inst TB Res, Coll Pharm, Chicago, IL USA
[3] Univ Autonoma Tamaulipas, Unidad Academ Multidisciplinaria Reynosa Rodhe, Ciudad Victoria, Mexico
[4] Univ Autonoma Chihuahua, Fac Ciencias Quim, Chihuahua, Mexico
[5] Univ Autonoma Benito Juarez Oaxaca, Fac Ciencias Quim, Lab Estudios Epidemiol Clin Disenos Expt & Invest, Oaxaca, Mexico
来源
RSC MEDICINAL CHEMISTRY | 2024年 / 15卷 / 08期
关键词
QUINOXALINE; CLOFAZIMINE;
D O I
10.1039/d4md00221k
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 mu M). 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 mu M 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.
引用
收藏
页码:2785 / 2791
页数:7
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