Application of Huisgen (3+2) cycloaddition reaction: Synthesis of 1-(2,3-dihydrobenzofuran-2-yl-methyl [1,2,3]-triazoles and their antitubercular evaluations

作者：Tripathi Rama P^*; Yadav Amit Kumar; Ajay Arya; Bisht Surendra Singh; Chaturvedi Vinita; Sinha Sudhir Kumar

来源：European Journal of Medicinal Chemistry, 2010, 45(1): 142-148.

DOI：10.1016/j.ejmech.2009.09.036

• 1,2,3-Triazoles
• [3+2] cycloaddition
• Cuprous iodide
• Antitubercular agents

1,4-Disubstituted-1,2,3-triazoles (3-27) have been synthesized by [3+2] cycloaddition of different 2-(azidomethyl)-dihydronaptho(benzo)furans (2a, 2b, 2c and 2d) with different alkynes. All the compounds were screened for antitubercular activity against Mycobacterium tuberculosis H(37)Rv. Compounds 2a, 7,9,12 and 14 exhibited antitubercular activities with MIC ranging from 12.5 to 3.12 mu g/ml.

• 出版日期2010-1