A5064744057- Asymmetric Synthesis and Catalysis
- Fluorine in Organic Chemistry
- Synthesis and Catalytic Reactions
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Cyclopropane Reaction Mechanisms
- Luminescence and Fluorescent Materials
- Carbohydrate Chemistry and Synthesis
- Molecular Sensors and Ion Detection
- Synthetic Organic Chemistry Methods
- Axial and Atropisomeric Chirality Synthesis
- Chemical synthesis and alkaloids
- Pesticide Residue Analysis and Safety
- Mathematics, Computing, and Information Processing
- Sulfur-Based Synthesis Techniques
- Enzyme Catalysis and Immobilization
- Mass Spectrometry Techniques and Applications
- Asymmetric Hydrogenation and Catalysis
- Pain Mechanisms and Treatments
- Chromium effects and bioremediation
- Organic and Inorganic Chemical Reactions
- Medical Imaging Techniques and Applications
- Human-Animal Interaction Studies
- Catalytic C–H Functionalization Methods
- Biochemical and Structural Characterization
Centre National de la Recherche Scientifique
2006-2024
Université de Rouen Normandie
2009-2024
Laboratoire COBRA
2015-2024
Normandie Université
2015-2024
Institut National des Sciences Appliquées Rouen Normandie
2006-2024
Différenciation et Communication Neuronale et Neuroendocrine
2023
Génétique Moléculaire Génomique Microbiologie
2006-2018
A general access to challenging and unprecedented C(sp)–, C(sp<sup>2</sup>)– C(sp<sup>3</sup>)–SCF<sub>2</sub>PO(OEt)<sub>2</sub> bonds <italic>via</italic> a BiCl<sub>3</sub> mediated transformation.
Fluorescent coumarins are an important class of small-molecule organic fluorophores ubiquitous in different well-established and emerging fields research including, among others, biochemistry chemical biology. The present work aims at covering the poor detectability coumarin-based conjugates by mass spectrometry while keeping photophysical properties coumarin core. In this context, synthesis readily functionalizable phosphonium-tagged derivatives enabling a dual mass-tag fluorescence...
This work aims at exploiting both the enantioselective Tsuji allylation of allyl carbonate 6 and an organocatalytic aza-ene-type domino reaction between enal 3a β-enaminone 4a to develop a straightforward access all four possible stereoisomers donepezil-like 1,4-dihydropyridine 1a (er up 99.5:0.5; overall yield 64%), anti-Alzheimer's prodrug candidate. strategy was extended preparation other enantioenriched 1,4-dihydropyridines 1b–i (eight examples), highlighting its potential in development...
Endomorphins, endogenous μ ‐opioid receptor ligands, have been shown to exert antinociceptive, antidepressant, anxiolytic, and neuromodulatory effects, as well influence cardiovascular, respiratory, gastrointestinal systems. In the present study, we designed synthesized a series of tetrapeptides tripeptides (amides peptide acids) similar endomorphins structure, but with low affinity, tested them possible inhibitors endomorphin‐degrading enzymes. The obtained results indicate that...
Proteins are able to irreversibly assemble biologically active ligands from building blocks bearing complementary reactive functions due their spatial proximity, through a kinetic target-guided synthetic process (also named in situ click chemistry). Although linkages thus formed mostly passive, some of them have shown significantly contribute the protein binding for instance hydrogen bonding and stacking interactions. Biocompatible reactions chemistry formidable source inspiration developing...
Efficient metal catalyzed C⁻H arylation of 8-alkyl-thiazolo[5,4-f]-quinazolin-9-ones was explored for SAR studies. Application this powerful chemical tool at the last stage synthesis kinase inhibitors allowed arrays molecules inspired by fragment-growing studies generated molecular modeling calculations. Among potentially active compounds designed through strategy, FC162 (4c) exhibits nanomolar IC50 values against some kinases, and is best candidate development as a DYRK inhibitor.
Maleimide-based Diels–Alder strategies for bioconjugation are compared in terms of dienes accessibility and stability, reactions rates, as well products isolation stability.
Photochemical hazes are expected to form and significantly contribute the chemical radiative balance of exoplanets with relatively moderate temperatures, possibly in habitable zone their host star. In presence humidity, haze particles might thus serve as cloud condensation nuclei trigger formation water droplets. present work, we interested impact such a close interaction between photochemical humidity on organic content composing capacity generate molecules high prebiotic potential. For...
An expeditious synthesis of taurine derivatives though a key unprecedented organocatalyzed enantioselective sulfa-Michael addition bisulfite onto nitrostyrenes.
We showcase the successful combination of photochemistry and kinetic target-guided synthesis (KTGS) for rapidly pinpointing enzyme inhibitors. KTGS is a fragment-based drug discovery (FBDD) methodology in which biological target (BT) orchestrates construction its own ligand from fragments featuring complementary reactive functionalities. Notably, interacting with protein binding sites leverage their spatial proximity, facilitating preferential reaction. Consequently, resulting bivalent...
Abstract We showcase the successful combination of photochemistry and kinetic target‐guided synthesis (KTGS) for rapidly pinpointing enzyme inhibitors. KTGS is a fragment‐based drug discovery (FBDD) methodology in which biological target (BT) orchestrates construction its own ligand from fragments featuring complementary reactive functionalities. Notably, interacting with protein binding sites leverage their spatial proximity, facilitating preferential reaction. Consequently, resulting...
Enantiomerization of allylic trifluoromethyl sulfoxides occurs spontaneously at room temperature through the corresponding trifluoromethanesulfenates via a [2,3]-sigmatropic rearrangement. Dynamic enantioselective high-performance liquid chromatography (HPLC) analysis revealed stereodynamics these ranging from chromatographic resolution to peak coalescence temperatures between 5 and 53 °C. The rate constant enantiomerization activation parameters were determined compared with Density...
Nine- and ten-membered lactones with up to three non-vicinal stereocenters (up 99 : 1 er dr) were prepared by ring expansion of prochiral alcohols (21 examples) upon exposure quinidine derivatives.
L’objectif de cette étude préliminaire était d’étudier l’impact trois séances médiation animale par le chien sur caregiving six mères détenues avec leur bébé au sein la nurserie d’une maison d’arrêt. Les résultats préliminaires ont montré une tendance à l’augmentation du sentiment compétence parentale et des occurrences comportements soin mères. Cela pourrait s’expliquer rôle support social que jouerait chien, améliorant santé psychique engendrant un meilleure qualité. Par ailleurs,...
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