title: Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis.
abstract: 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.
authors: Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625 021, Tamil Nadu, India.
authors: Poovan
authors: P
authors: Shanmugavelan
authors: Sangaraiah
authors: S
authors: Nagarajan
authors: Murugan
authors: M
authors: Sathishkumar
authors: Alagusundaram
authors: A
authors: Ponnuswamy
authors: Perumal
authors: P
authors: Yogeeswari
authors: Dharmarajan
authors: D
authors: Sriram
mesh_terms: D000480:Alkynes / Q000737:chemistry; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001386:Azides / Q000737:chemistry; D005231:Fatty Acids, Unsaturated / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000480:Alkynes; D000995:Antitubercular Agents; D001386:Azides; D005231:Fatty Acids, Unsaturated; D014230:Triazoles; C024060:2-butynedioic acid