abstract |
Disclosed are a benzothiazinone derivative, a preparation method therefor and use thereof as an anti-tuberculosis drug. The present invention specifically relates to a new class of compounds having a benzothiazinone skeleton. Such compounds show an inhibitory effect on mycobacterium tuberculosis, and in particular, an inhibitory effect also on mycobacterium tuberculosis having clinical drug resistance. Compared with the existing clinical first-line drug isoniazide (MIC 0.5μM), the activity of such compounds has a great advantage; compared with the existing benzothiazinone antituberculosis drug pBTZ 169 at the research stage, such compounds have a lower cLogP value, and has better druggability. |