Aim. The aim of our study was to develop small–molecular inhibitors of M. tuberculosis LeuRS with antibacterial activity. Conclusions. Using in silico approaches we identified several chemical classes of inhibitors targeting M. tuberculosis LeuRS and MetRS with IC₅₀ values in micromolar concentration range. It was found that the most promising compounds which possess antibacterial activity belong to N–benzylidene–N’–thiazol–2–yl–hydrazine derivatives. Therefore, the compounds in this class can be valuable for further biological research and optimization.