A5079834887- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and biological activity
- Cancer Mechanisms and Therapy
- Chemical Synthesis and Analysis
- Biochemical Acid Research Studies
- Enzyme Structure and Function
- Infections and bacterial resistance
- Click Chemistry and Applications
- Carbohydrate Chemistry and Synthesis
- Antibiotic Resistance in Bacteria
- Biochemical and Molecular Research
- Catalytic Cross-Coupling Reactions
- Synthetic Organic Chemistry Methods
- Enzyme Catalysis and Immobilization
- Synthesis and Characterization of Heterocyclic Compounds
- Quinazolinone synthesis and applications
- Bacterial biofilms and quorum sensing
- Cancer therapeutics and mechanisms
- Pneumocystis jirovecii pneumonia detection and treatment
- Bioactive Compounds and Antitumor Agents
- Enzyme Production and Characterization
- Cyclopropane Reaction Mechanisms
- Phytochemical compounds biological activities
- Synthesis and bioactivity of alkaloids
Institut de Chimie de Clermont-Ferrand
2015-2024
Université Clermont Auvergne
2015-2024
Centre National de la Recherche Scientifique
2015-2024
Sigma Clermont
2017-2020
Sapienza University of Rome
2019
Institut de Biologie Structurale
2005-2017
CEA Grenoble
2005-2017
Commissariat à l'Énergie Atomique et aux Énergies Alternatives
2005-2017
Université Grenoble Alpes
2005-2017
Université Joseph Fourier
2005-2017
Understanding the mechanisms influencing poly(ethylene terephthalate) (PET) biodegradation is crucial for developing innovative strategies to accelerate breakdown of this persistent plastic. In study, we employed all-atom molecular dynamics simulation investigate adsorption process LCC-ICCG cutinase enzyme onto PET surface. Our results revealed that hydrophobic, π–π, and H bond interactions, specifically involving aliphatic, aromatic, polar uncharged amino acids, were primary driving forces...
The synthesis of new meridianin derivatives is described. indolic ring system was substituted at the C-4 to C-7 positions either by a bromine atom or nitro amino groups. Additionally, an iodine various aryl groups were introduced C-5 position 2-aminopyrimidine ring. These compounds as well some their synthetic intermediates tested for kinase inhibitory potencies and in vitro antiproliferative activities. We found that this series particularly interesting development inhibitors DYRK1A CLK1...
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...
Abstract Copper(I)‐catalysed azide–alkyne cycloaddition (CuAAC) has been successfully conducted under reductant‐free conditions. The catalytic system consisted of a combination copper(I)–N‐heterocyclic carbene complex and aromatic N‐donors. catalyst is stable can be stored, thus rendering the reaction valuable for routine use.
Transketolase variants catalyse a promiscuous acyloin condensation of aliphatic aldehydes leading in one step to unsymmetrical α-hydroxyketones while offering green advances compared previous enzymatic and chemical ways.
A platinum Chugaev complex was synthesised and fully characterized by multinuclear NMR spectroscopy X-ray crystallography. This cis bis acyclic diamino carbene acts as a cytotoxic compound behaves cisplatin equivalent interacting with supercoiled DNA thiols. Stability of the ligand is also discussed.
Abstract Transketolase (TK) from various origins (including Escherichia coli and yeast) has been described to be fully enantiomer specific for (2 R )‐hydroxyaldehyde substrates. A thermostable TK G eobacillus stearothermophilus (TK gst ) was found display a minor reactivity S )‐hydroxylated aldehydes. To improve this activity by directed protein evolution, we have built library of variants site saturation mutagenesis on two key positions L382 D470. The best double mutant L382D/D470S shows up...
The head-to-tail macrocyclisation of arylopeptoids (oligomeric <italic>N</italic>-substituted aminomethyl benzamides) has enabled the first X-ray structures arylopeptoid constructs and identification well-defined architectures in solution.
Abstract Water‐soluble gold(III/I) N‐heterocylic carbene complexes behave as efficient catalysts for the hydration of terminal alkynes in neat water. The transformation proceeds absence Brønsted acids or halide scavengers and is suitable sensitive substrates. Kinetic profiles DFT studies provide a clear picture intermediates present during catalysis. magnified image
Abstract Dihydroxyacetone phosphate (DHAP)‐dependent rhamnulose aldolases display an unprecedented versatility for ketones as electrophile substrates. We selected and characterized a aldolase from Bacteroides thetaiotaomicron (RhuABthet) to provide proof of concept. DHAP was added nucleophile several α‐hydroxylated used electrophiles. This aldol addition stereoselective produced branched‐chain monosaccharide adducts with tertiary alcohol moiety. Several aldols were readily obtained in good...
A new strategy was developed for the modification of silver(I) and gold(I) N-heterocyclic carbenes. Azido groups were grafted used either by copper-catalysed azide–alkyne cycloaddition before metallation or thermal "strain-promoted" 1,3-dipolar after to functionalise metal-NHCs.
Tertiary alcohols are widely represented in nature and among bioactive molecules. Their importance is attested by the continuous efforts to meet challenge of their stereoselective synthesis. In this context, we propose an enzymatic approach, involving class II pyruvate aldolases. These enzymes shown catalyze selective cross-aldol reactions between pyruvic acid or derivatives as nucleophiles a series ketones electrophiles. This catalytic activity exemplified highly preparation seven branched...
Abstract Complexes of the type [PdX(PPh 3 )( 1 )]X [ = 4‐phenyl‐3‐thiosemicarbazide; X Cl – ( 2 ), Br I 4 and SCN 5 )] have been synthesized characterized by elemental analyses IR, UV/Vis, H 13 C NMR spectroscopy. The molecular structure complex was determined single‐crystal X‐ray diffraction. binding complexes with a purine base (guanosine) investigated spectroscopy mass spectrometry, which showed to coordinate guanosine through N7. A gel electrophoresis assay demonstrated ability cleave...
We propose an ecofriendly, efficient, stereoselective procedure for the two-carbon elongation of nonphosphorylated aldoses (C4–C6) to corresponding Cn+2 ketoses (C6–C8) in one step, using hydroxypyruvate (HPA) as a ketol donor substrate and evolved thermostable transketolase from Geobacillus stearothermophilus (TKgst) biocatalyst. Simultaneous site saturation mutagenesis (SSM) at two or three key positions TKgst active yielded efficient variants, L382F/F435Y, R521Y/S385/H462N,...
Abstract Triazole chelators, synthesized by click chemistry, are convenient ligands for palladium(II) and platinum(II). Conformational changes induced the complexation of these Pd II Pt complexes with guanosine similar to those cisplatin. In addition, behave like cisplatin regard relaxation supercoiled plasmid DNA.
N-(2-Azidophenyl)azolium salts were easily prepared and reacted with copper(i) under conditions allowing the formation of NHC complexes. Under these conditions, benzimidazo-fused heterocycles occurred catalytic, efficient very mild conditions. This reaction is proposed to proceed via dinitrogen elimination imido/nitrene-NHC cyclization.