1. A novel benzothiazinethione analogue SKLB-TB1001 displays potent antimycobacterial activities in a series of murine models.
- Author
-
Gao C, Ye TH, Peng CT, Shi YJ, You XY, Xiong L, Ran K, Zhang LD, Zeng XX, Wang NY, Yu LT, and Wei YQ
- Subjects
- Animals, Colony Count, Microbial, Disease Models, Animal, Female, Lung drug effects, Lung microbiology, Lung pathology, Mice, Inbred BALB C, Mice, Inbred C57BL, Survival Analysis, Thiadiazoles chemical synthesis, Thiadiazoles chemistry, Thiadiazoles therapeutic use, Treatment Outcome, Tuberculosis drug therapy, Tuberculosis microbiology, Tuberculosis pathology, Antitubercular Agents pharmacology, Mycobacterium tuberculosis drug effects, Thiadiazoles pharmacology
- Abstract
New chemotherapeutic compounds and regimens are needed to combat multidrug-resistant Mycobacterium tuberculosis. Here, we used a series of murine models to assess an antitubercular lead compound SKLB-TB1001. In the Mycobacterium bovis bacillus Calmette-Guérin and the acute M. tuberculosis H37Rv infection mouse models, SKLB-TB1001 significantly attenuated the mycobacterial load in lungs and spleens. The colony forming unit counts and histological examination of lungs from H37Rv infected mice revealed that the benzothiazinethione analogue SKLB-TB1001 as a higher dose level was as effective as isoniazid. Moreover, in a multidrug-resistant (MDR)-TB mouse model, SKLB-TB1001 showed significant activity in a dose-dependent manner and was more effective than streptomycin. These results suggested that SKLB-TB1001 could be an antitubercular drug candidate worth further investigation., (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)
- Published
- 2017
- Full Text
- View/download PDF