Design and Synthesis of Some New 3-Oxo/thioxo-1,2,4-triazolo[4,3-a]benzimidazole Derivatives Bearing a 4-Tollyl Sulfonyl Moiety as Antimycobacterial Agents

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)-N²-(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.

Graphical Abstract

Keywords:

• Antimycobacterium
• synthesis
• 1,2,4-triazolo[4,3-a]benzimidazoles

Acknowledgments

The authors would like to thank the Chemistry Department at King Abdulaziz University, Jeddah, for supporting this Research. Thanks to Prof Reda Abdel-Rahman (D.Sc. Organic chemistry), for his help and constant support.

Disclosure statement

The authors confirm that this article content has no conflict of interest.