High susceptibility of MDR and XDR Gram-negative pathogens to biphenyl-diacetylene-based difluoromethyl-allo-threonyl-hydroxamate LpxC inhibitors.
Fiche publication
Date publication
octobre 2016
Journal
The Journal of antimicrobial chemotherapy
Auteurs
Membres identifiés du Cancéropôle Est :
Pr HOCQUET Didier
Tous les auteurs :
Titecat M, Liang X, Lee CJ, Charlet A, Hocquet D, Lambert T, Pagès JM, Courcol R, Sebbane F, Toone EJ, Zhou P, Lemaitre N
Lien Pubmed
Résumé
Inhibitors of uridine diphosphate-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC, which catalyses the first, irreversible step in lipid A biosynthesis) are a promising new class of antibiotics against Gram-negative bacteria. The objectives of the present study were to: (i) compare the antibiotic activities of three LpxC inhibitors (LPC-058, LPC-011 and LPC-087) and the reference inhibitor CHIR-090 against Gram-negative bacilli (including MDR and XDR isolates); and (ii) investigate the effect of combining these inhibitors with conventional antibiotics.
Mots clés
Acinetobacter baumannii, drug effects, Amidohydrolases, antagonists & inhibitors, Anti-Bacterial Agents, pharmacology, Bacterial Proteins, biosynthesis, Drug Resistance, Multiple, Bacterial, Enterobacteriaceae, drug effects, Enterobacteriaceae Infections, microbiology, Enzyme Inhibitors, pharmacology, Escherichia coli, drug effects, Gram-Negative Bacteria, drug effects, Humans, Hydroxamic Acids, pharmacology, Klebsiella pneumoniae, drug effects, Microbial Sensitivity Tests, Pseudomonas aeruginosa, drug effects, Threonine, analogs & derivatives, beta-Lactamases, biosynthesis
Référence
J. Antimicrob. Chemother.. 2016 10;71(10):2874-82