Synthesis and evaluation of 1-alkyl-4-phenyl-[1,2,3]-triazole derivatives as antimycobacterial agent

Fourteen small molar mass 1-alkyl-4-phenyl-[1,2,3]-triazole derivatives were prepared using a straightforward and efficient method for the regioselective synthesis of [1,2,3]-triazoles and the compounds were screened for antimycobacterial activity against multiple-drug-resistant strains of Mycobacterium tuberculosis H37Rv. The synthetic methodology consisted of a Cu(I)-catalyzed 1,3-dipolar cycloaddition of aryl azides to terminal arylacetylenes (click-reaction). Six [1,2,3]-triazoles were found to be more active against M. tuberculosis than the positive control ethambutol.

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Bibliographic Details
Main Authors: Gallardo,Hugo, Conte,Gilmar, Bryk,Fernando, Lourenço,Maria Cristina S., Costa,Marilia S., Ferreira,Vitor F.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2007
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532007000600027
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