1345823-29-1Relevant articles and documents
Synthesis and evaluation of α-ketotriazoles and α,β- diketotriazoles as inhibitors of Mycobacterium tuberculosis
Menendez, Christophe,Rodriguez, Frédéric,Ribeiro, Ana Luisa De Jesus Lopes,Zara, Francesca,Frongia, Céline,Lobjois, Valérie,Saffon, Nathalie,Pasca, Maria Rosalia,Lherbet, Christian,Baltas, Michel
, p. 167 - 173 (2013/10/01)
Two series of α-ketotriazole and α,β-diketotriazole derivatives were synthesized and evaluated for antitubercular and cytotoxic activities. Among them, two α,β-diketotriazole compounds, 6b and 9b, exhibited good activities (minimum inhibitory concentratio
Synthesis of α,β-diketotriazoles by aerobic copper-catalyzed oxygenation with triazole as an intramolecular assisting group
Menendez, Christophe,Gau, Sylvain,Ladeira, Sonia,Lherbet, Christian,Baltas, Michel
experimental part, p. 409 - 416 (2012/02/04)
The catalytic oxidation of α-ketotriazoles to α,β- diketotriazoles was performed with CuCl2 or CuI/2,9-dimethyl-1,10- phenanthroline in air at 80 °C in good yields. Studies showed that the triazole group participates in complexation to the copper and favors oxidation. Copyright
Synthesis and biological activities of triazole derivatives as inhibitors of InhA and antituberculosis agents
Menendez, Christophe,Gau, Sylvain,Lherbet, Christian,Rodriguez, Frédéric,Inard, Cyril,Pasca, Maria Rosalia,Baltas, Michel
, p. 5524 - 5531 (2011/12/15)
InhA, the enoyl reductase from the mycobacterial type II fatty acid biosynthesis pathway, is a target for the development of novel drugs against tuberculosis. We exploited copper-catalyzed [3+2] cycloaddition between alkynes and different azides to afford 1,4-disubstituted triazole or α-ketotriazole derivatives. Several compounds bearing a lipophilic chain mimicking the substrate were able to inhibit InhA. Among them, 1-dodecyl-4-phenethyl-1H-1,2,3-triazole displayed a minimum inhibitory concentration inferior to 2 μg/mL against Mycobacterium tuberculosis H37Rv.