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Eur J Med Chem ; 46(11): 5524-31, 2011 Nov.
Article in English | MEDLINE | ID: mdl-21944473

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.


Subject(s)
Bacterial Proteins/antagonists & inhibitors , Chemistry Techniques, Synthetic , Mycobacterium tuberculosis/drug effects , Mycobacterium tuberculosis/enzymology , Oxidoreductases/antagonists & inhibitors , Triazoles/chemical synthesis , Triazoles/pharmacology , Antitubercular Agents/chemical synthesis , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Bacterial Proteins/chemistry , Catalytic Domain , Drug Design , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Microbial Sensitivity Tests , Models, Molecular , Oxidoreductases/chemistry , Triazoles/chemistry , Triclosan/chemistry
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