Publications (25) View all
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Article: Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.
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ABSTRACT: A series of triazoles have been prepared and evaluated as inhibitors of InhA as well as inhibitors of Mycobacterium tuberculosis H(37)R(v). Several of these new compounds possess a good activity against InhA, particularly compounds 17 and 18 for which molecular docking has been performed. Concerning their activities against M. tuberculosis H(37)R(V) strain, two of them, 3 and 12, were found to be good inhibitors with MIC values of 0.50 and 0.25 μg/mL, respectively. Particularly, compound 12 presenting the best MIC value of all compounds tested (0.6 μM) is totally inactive against InhA.European journal of medicinal chemistry 03/2012; 52:275-83. · 3.27 Impact Factor -
Article: Synthesis of α,β-Diketotriazoles by Aerobic Copper-Catalyzed Oxygenation with Triazole as an Intramolecular Assisting Group
European Journal of Organic Chemistry 01/2012; · 3.33 Impact Factor -
Article: Synthesis and biological activities of triazole derivatives as inhibitors of InhA and antituberculosis agents.
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ABSTRACT: 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.European journal of medicinal chemistry 09/2011; 46(11):5524-31. · 3.27 Impact Factor -
Article: New potent bisubstrate inhibitors of histone acetyltransferase p300: design, synthesis and biological evaluation.
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ABSTRACT: Bisubstrate-type compound Lys-CoA has been shown to inhibit the p300 histone acetyl transferase activity efficiently and may constitute a lead compound for a novel class of anticancer therapeutics. Based on this strategy, we synthesized a series of CoA derivatives and evaluated these molecules for their activity as p300 histone acetyltransferases inhibitor. The best activity was obtained with compound 3 bearing a C-5 spacing linker that connects the CoA moiety to a tert-butyloxycarbonyl (Boc) group. Based on docking simulations, this inhibitor exhibits favorable interactions with two binding areas, namely pockets P1 and P2, within the active site.Chemical Biology & Drug Design 01/2011; 77(1):86-92. · 2.28 Impact Factor -
Article: Bismuth Triflate as a Safe and Readily Handled Source of Triflic Acid: Application to the Oxa-Pictet-Spengler Reaction
Synthetic Communications 01/2010; 40:915-926. · 1.06 Impact Factor
