THE SYNTHESIS OF 1-OXA-9-AZASPIRO[5.5]UNDECANE DERIVATIVES AND OPTIMIZATION OF ANTITUBERCULOSIS ACTIVITY THEREOF
Keywords:
1-oxa-9-azaspiro[5.5]undecane, spirocyclic compounds, antituberculosis activity, MmpL3 protein, Prins cyclizationAbstract
The aim of this work was to synthesize and study the antituberculosis activity of spirocyclic inhibitors of the MmpL3 protein of M. tuberculosis containing the 1-oxa-9-azaspiro[5.5]undecane scaffold. Optimization of the initial structure was performed with consideration of the results of molecular docking. The resulting compounds, characterized by the chemical diversity of the peripheral fragment, showed high activity against the antibiotic-sensitive strain H37Rv and some multiresistant strains of M. tuberculosis, exceeding the activity of the comparator drug.
![](https://hgs.osi.lv/public/journals/1/submission_8965_7799_coverImage_en_US.png)
Downloads
Additional Files
Published
2024-08-01
Issue
Section
Original Papers