Bioorganic & Medicinal Chemistry Letters 2011-12-15

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

Poovan Shanmugavelan, Sangaraiah Nagarajan, Murugan Sathishkumar, Alagusundaram Ponnuswamy, Perumal Yogeeswari, Dharmarajan Sriram

文献索引：Bioorg. Med. Chem. Lett. 21 , 7273-6, (2011)

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摘要

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 H(37)Rv strain. Four of the compounds showed MIC in the range of 1.56-3.13 μg/mL proving their potential activity.Copyright © 2011 Elsevier Ltd. All rights reserved.