A5015298513- Antibiotic Resistance in Bacteria
- Pneumocystis jirovecii pneumonia detection and treatment
- Tuberculosis Research and Epidemiology
- Organophosphorus compounds synthesis
- Synthesis and biological activity
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Cancer Mechanisms and Therapy
- Asymmetric Hydrogenation and Catalysis
- Synthesis of β-Lactam Compounds
- Synthesis and Reactivity of Heterocycles
- Regulation of Appetite and Obesity
- Bioactive Compounds and Antitumor Agents
- Chemical Synthesis and Analysis
- Phosphorus compounds and reactions
- Chemical Reactions and Isotopes
- HIV/AIDS drug development and treatment
- Phenothiazines and Benzothiazines Synthesis and Activities
- Computational Drug Discovery Methods
- Biochemical Analysis and Sensing Techniques
- Catalytic C–H Functionalization Methods
- Chemical Reaction Mechanisms
- Synthesis and pharmacology of benzodiazepine derivatives
- Receptor Mechanisms and Signaling
- Synthesis and bioactivity of alkaloids
Centre National de la Recherche Scientifique
2011-2024
Institut des Biomolécules Max Mousseron
2014-2024
Université de Montpellier
2015-2024
École Nationale Supérieure de Chimie de Montpellier
2017-2024
Texas Christian University
2012-2014
Institut de Chimie de Clermont-Ferrand
2013-2014
Université Clermont Auvergne
2010-2014
Molécules d'Intérêt Biologique
2010-2011
Université de Lille
2010-2011
Université Lille Nord de France
2010-2011
Significance G protein-coupled receptors (GPCRs), one of the largest cell surface receptor families, transmit their signals through coupling intracellular partners, such as proteins. Knowing how this occurs is essential, because it governs entire signaling process. To address open question, we used a purified GPCR model to which applied various state-of-the-art biochemical and biophysical approaches. By doing so, provide direct experimental evidence mechanism in conformational changes are...
Ghrelin plays a central role in controlling major biological processes. As for other G protein-coupled receptor (GPCR) peptide agonists, the structure and dynamics of ghrelin bound to its remain obscure. Using combination solution-state NMR molecular modeling, we demonstrate that binding growth hormone secretagogue is accompanied by conformational change structures region, involving formation well-defined hydrophobic core. By comparing acylated nonacylated forms, conclude octanoyl chain...
Abstract Metallo‐β‐lactamases (MBLs) cause resistance of Gram‐negative bacteria to β‐lactam antibiotics and are serious concern, because they can inactivate the last‐resort carbapenems MBL inhibitors clinical value still lacking. We previously identified original binding mode 4‐amino‐2,4‐dihydro‐5‐(2‐methylphenyl)‐3 H ‐1,2,4‐triazole‐3‐thione (compound IIIA) within dizinc active site L1 MBL. Herein we present crystallographic structure a complex with corresponding non‐amino compound IIIB...
Herein, we describe a new methodology for selective cephalosporin functionalization at the C3 position. First an optimization study reaction conditions is performed and allowed to define favorable parameters...
Metallo-β-lactamases (MBLs) contribute to the resistance of Gram-negative bacteria carbapenems, last-resort antibiotics at hospital, and MBL inhibitors are urgently needed preserve these important antibacterial drugs. Here, we describe a series 1,2,4-triazole-3-thione-based displaying an α-amino acid substituent, which amine was mono- or disubstituted by (hetero)aryl groups. Compounds certain nitrogen-containing heterocycles showed submicromolar activities against VIM-type enzymes strong...
(Hydroxymethyl)phosphorus compounds are well-known and valuable in general; however the use of (hydroxymethyl)phosphinates R1P(O)(OR2)CH2OH particular has been much more limited. The potential this functionality not yet fully realized because mild unmasking hydroxymethyl group was available. oxidative conversion into R1P(O)(OR2)H using Corey–Kim oxidation is described. Other reactions preserving methylene carbon also reported.
Abstract Metallo‐β‐lactamases (MBLs) are increasingly involved as a major mechanism of resistance to carbapenems in relevant opportunistic Gram‐negative pathogens. Unfortunately, clinically efficient MBL inhibitors still represent an unmet medical need. We previously reported several series compounds based on the 1,2,4‐triazole‐3‐thione scaffold. In particular, Schiff bases formed between diversely 5‐substituted‐4‐amino and 2‐carboxybenzaldehyde were broad‐spectrum VIM‐type, NDM‐1 IMP‐1...
To fight the increasingly worrying bacterial resistance to antibiotics, discovery and development of new therapeutics is urgently needed. Here, we report on a series 1,2,4-triazole-3-thione compounds as inhibitors metallo-β-lactamases (MBLs), which represent major determinants β-lactams, especially carbapenems, in Gram-negative bacteria. These molecules are stable analogs 4-amino-1,2,4-triazole-derived Schiff bases, where hydrazone-like bond has been reduced (hydrazine series) or 4-amino...
In the context of SIBFA polarizable molecular mechanics/dynamics (PMM/PMD) procedure, we report calibration and a series validation tests for 1,2,4-triazole-3-thione (TZT) heterocycle. TZT acts as chelating group inhibitors dizinc metallo-β-lactamases (MBL), an emerging class Zn-dependent bacterial enzymes, which by cleaving β-lactam bond most antibiotics are responsible acquired resistance bacteria to these drugs. Such study is indispensable prior performing PMD simulations complexes...
Addressing antibacterial resistance is a major concern of the modern world. The development new approaches to meet this deadly threat critical priority. In article, we investigate approach negate bacterial resistance: exploit β-lactam bond cleavage by β-lactamases selectively trigger prodrugs into periplasm. Indeed, multidrug-resistant Gram-negative pathogens commonly produce several that are able inactivate antibiotics, our most reliable and widely used therapeutic option. chemical...