Bioorganic and Medicinal Chemistry Letters p. 7273 - 7276 (2011)
Update date:2022-08-04
Topics: In vitro Antitubercular activity Efficient Synthesis Mycobacterium tuberculosis 1,2,3-triazoles
Shanmugavelan, Poovan
Nagarajan, Sangaraiah
Sathishkumar, Murugan
Ponnuswamy, Alagusundaram
Yogeeswari, Perumal
Sriram, Dharmarajan
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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