Detalle Publicación

ARTÍCULO
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis
Título de la revista: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS
ISSN: 0960-894X
Volumen: 26
Número: 9
Páginas: 2188 - 2193
Fecha de publicación: 2016
Resumen:
Twenty-four quinoxaline derivatives were evaluated for their antimycobacterial activity using BacTiter-Glo microbial cell viability assay. Five compounds showed MIC values < 3.1 mu M and IC50 values < 1.5 mu M in primary screening and therefore, they were moved on for further evaluation. Compounds 21 and 18 stand out, showing MIC values of 1.6 mu M and IC50 values of 0.5 and 1.0 mu M, respectively. Both compounds were the most potent against three evaluated drug-resistant strains. Moreover, they exhibited intracellular activity in infected macrophages, considering log-reduction and cellular viability. In addition, compounds 16 and 21 were potent against non-replicating Mycobacterium tuberculosis and compound 21 was bactericidal. Therefore, quinoxaline derivatives could be considered for making further advances in the future development of antimycobacterial agents.