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

Journal of the Brazilian Chemical Society

Hugo Gallardo²  Gilmar Conte²  Fernando Bryk²  Maria Cristina S. Lourenço¹  Marilia S. Costa¹  Vitor F. Ferreira¹ 

[1] ,Universidade Federal de Santa Catarina Departamento de Química Florianópolis SC ,Brazil

关键词: tuberculosis;    click reaction;    1;    2;    3-triazoles;   

DOI  :  10.1590/S0103-50532007000600027

来源: SciELO

【 摘 要 】

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.

【 授权许可】

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