Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis

Efficient and rapid synthesis of 1,2,3-triazole derivatives has been achieved via Huisgen’s 1,3-dipolar cycloaddition between alkyl/arylazides and diethyl/dimethyl acetylenedicarboxylate in excellent yields under solvent-free conditions. The environmentally friendly solvent-free protocol overcomes the limitations associated with the prevailing time-consuming solution phase protocols and affords the triazoles just in 1–3 min. In vitro antitubercular activity of these triazoles was screened against Mycobacterium tuberculosis H37Rv strain. Four of the compounds showed MIC in the range of 1.56–3.13 μg/mL proving their potential activity.

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