The preparation of a series of new 2-aminoaryl-1, 3, 4-thiadiazoles substituted with methylsulfanyl, methansulfinyl, or amine in the 5-position is described in this article. The compounds were obtained from N-hydroxyimidoyl chlorides and methyl dithiocarbazinate or 4-substituted thiosemicarbazides in a thermal 1, 3-dipolar cycloaddition reaction. The new derivatives were tested for their activity against Mycobacterium tuberculosis.