A number of new 3-alkylthio-6-(3,5-dimethylpyrazol-1-yl)[1,2,4]triazolo[4,3-b][1,2,4,5]-tetrazines were synthesized and modified in nucleophilic substitution reactions with aliphatic amines. The study of the tuberculostatic activity of the compounds obtained revealed a number of active derivatives with a minimum inhibitory concentration of 0.37-3.1 µg mL-1.