• Publications
  • Influence
Hydroxamic Acids as Potent Inhibitors of FeII and MnII E. coli Methionine Aminopeptidase: Biological Activities and X‐ray Structures of Oxazole Hydroxamate–EcMetAP‐Mn Complexes
TLDR
Increased antibacterial activity was observed mainly for compounds with a 2‐substituted phenyl group in the presence of the nonapeptide polymyxin B and phenylalanine–arginine–β‐naphthylamide as permeabilizer and efflux pump blocker, respectively, which boost the intracellular uptake of the inhibitors. Expand
Suppression-Subtractive Hybridization as a Strategy To Identify Taxon-Specific Sequences within the Mycoplasma mycoides Cluster: Design and Validation of an M. capricolum subsp. capricolum-Specific
TLDR
Due to a high intrataxon polymorphism and important cross-reactions between taxa, a single DNA fragment was shown to be specific for M. capricolum among other mycoplasmas, including all members of the M. mycoides cluster. Expand
Conjugation of a new series of dithiocarbazate Schiff base Copper(II) complexes with vectors selected to enhance antibacterial activity.
TLDR
These Cu(II)-R9 derivatives display remarkable antibacterial activity against a wide spectrum of bacteria and, in particular, are highly efficacious against Staphylococcus aureus with minimum inhibitory concentration (MIC) values of 0.5-1 μM. Expand
Fluoroquinolone structure and translocation flux across bacterial membrane
TLDR
This represents the first protocol to identify some structural parameters involved in antibiotic translocation and accumulation, and to illustrate the recently proposed “Structure Intracellular Concentration Activity Relationship” (SICAR) concept. Expand
Antibiotic Transport in Resistant Bacteria: Synchrotron UV Fluorescence Microscopy to Determine Antibiotic Accumulation with Single Cell Resolution
TLDR
To the first time that the intracellular accumulation of a clinical antibitiotic could be determined and discussed in relation with the level of drug susceptibility for a multiresistant strain, this method to non-invasively monitor the quinolones uptake in single bacteria is developed. Expand
In Vivo Evolution of Bacterial Resistance in Two Cases of Enterobacter aerogenes Infections during Treatment with Imipenem
TLDR
Genotype-phenotype correlations in Enterobacter aerogenes, a clinically problematic and antibiotic resistant bacterium, are described and a comprehensive analysis of membrane alterations relative to mutational steps in the evolution of MDR of a recognized nosocomial pathogen is provided. Expand
Microspectrometric insights on the uptake of antibiotics at the single bacterial cell level
TLDR
This technique represents a new method to assay drug translocation inside the cell and therefore incorporate rational drug design to impact antibiotic uptake, and seeks to identify pharmacophoric groups which improve penetration, and therefore accumulation, of small-molecule antibiotics inside bacteria. Expand
New Peptide-based antimicrobials for tackling drug resistance in bacteria: single-cell fluorescence imaging.
New peptide molecules with metal binding abilities proved to be active against multidrug resistant clinical isolates. One of them labeled with a dansylated lysine has been imaged insideExpand
1‐(1H‐Indol‐3‐yl)ethanamine Derivatives as Potent Staphylococcus aureus NorA Efflux Pump Inhibitors
TLDR
Structural–activity relationships studies revealed that the indolic aldonitrones halogenated at position 5 of the indole core were the most efficient inhibitors of the S. aureus NorA efflux pump, the highest reported to date for an indolic NorA inhibitor. Expand
Spectrofluorimetric quantification of antibiotic drug concentration in bacterial cells for the characterization of translocation across bacterial membranes.
TLDR
Three approaches that have been developed in the authors' laboratories to quantify drugs accumulated in intact cells by spectrofluorimetry, microspectro fluorimetric, and kinetics microspectrometry are described, which provide complementary results that highlight the contribution of membrane-associated mechanisms. Expand
...
1
2
3
...