Abstract
Some new 3-oxo/thioxo-1,2,4-triazolo[4,3-a]benzimidazole derivatives (3-13), bearing 4-tollyl sulfonyl moiety as bioactive probes, have been synthesized based on the cyclization of N '-(4-tollylfonyl)-N-2-(benzimidazole-2 '-yl)hydrazine with diethyl carbonate and/or carbon disulfide followed by alkylation, acylation, and/or aroylation reactions. The structure of the products is deduced from elemental analysis and spectral measurements. Furthermore, the new synthesized targets are evaluated as antimycobacterial agents. Compounds 13, 16, and 14 exhibit a high inhabitation activity towards the mycobacterium strain over the other tested compounds.