期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 9, 页码 2188-2193出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.066
关键词
Tuberculosis; Antimycobacterial; Quinoxaline; Intracellular activity
资金
- Division of Microbiology and Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Department of Health and Human Services [HHSN272201100009I]
- Government of Navarra
- University of Navarra
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. (C) 2016 Elsevier Ltd. All rights reserved.
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