A5046758081- Chemical synthesis and alkaloids
- Cholinesterase and Neurodegenerative Diseases
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Chemical Synthesis and Analysis
- Computational Drug Discovery Methods
- Axial and Atropisomeric Chirality Synthesis
- Nicotinic Acetylcholine Receptors Study
- Glioma Diagnosis and Treatment
- Asymmetric Synthesis and Catalysis
- Radiopharmaceutical Chemistry and Applications
- Synthetic Organic Chemistry Methods
- Synthesis of Organic Compounds
- Synthesis and Biological Evaluation
- Catalytic C–H Functionalization Methods
- Crystal structures of chemical compounds
- Alzheimer's disease research and treatments
- Phenothiazines and Benzothiazines Synthesis and Activities
- 14-3-3 protein interactions
- Multicomponent Synthesis of Heterocycles
- Conducting polymers and applications
- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Marine Sponges and Natural Products
- Click Chemistry and Applications
Normandie Université
2014-2024
Centre National de la Recherche Scientifique
2014-2024
Institut National des Sciences Appliquées Rouen Normandie
2014-2024
Laboratoire COBRA
2015-2024
Université de Rouen Normandie
2014-2024
Commissariat à l'Énergie Atomique et aux Énergies Alternatives
2017-2019
Université de Caen Normandie
2017-2019
Cyceron
2017
Babeș-Bolyai University
2007-2013
With the aim of reducing side effects acetylcholinesterase inhibitors (AChEIs) during symptomatic treatment Alzheimer's disease, we report herein a new class donepezil-based "bio-oxidizable" prodrugs 1 designed to be converted into dual binding site AChEIs 2. While most indanone-derived N-benzylpyridinium salts 2 revealed highly potent hAChEIs (IC50 up 3 nM), outperforming standard drug donepezil = 11 corresponding 1,4-dihydropyridines were found inactive. Promisingly, whereas selected...
<i>N</i>-Hydroxysuccinimide esters (NHS-esters) are important and widely used tools in various areas of chemistry including peptide synthesis, bioconjugate chemistry, functionalized materials polymers. The usual strategy employed to prepare these active generally relies on the coupling reaction with a carboxylic acid <i>N</i>-hydroxysuccinimide presence agent. However, more recently, many other efficient strategies have emerged literature. This short review covers literature devoted...
With the aim of improving efficiency marketed acetylcholinesterase (AChE) inhibitors in symptomatic treatment Alzheimer's disease, plagued by adverse effects arising from peripheral cholinergic activation, this work reports a biological evaluation new central AChE based on an original "bio-oxidizable" prodrug strategy. After injection 1a [IC50 > 1 mM (hAChE)] mice, monitoring markers and activation provided vivo proof-of-concept for brain delivery drug 2a = 20 nM through redox 1a....
An efficient Pd-catalyzed carbonylation protocol is described for the coupling of a large panel aryl, heteroaryl, benzyl, vinyl and allyl halides 2 with unusual N-hydroxysuccinimidyl (NHS) formate 1 as CO surrogate to afford corresponding valuable NHS esters 3. High conversion products was achieved up 98% yield by means Pd(OAc)2/Xantphos catalyst system.
Abstract Natural occurrence, synthesis, chemical behavior, and physical properties of aromatic cyclopenta[ c ]pyrans are reviewed. Various strategies for the synthesis starting from cyclopentadienes, fulvenes, oxadiazinones, or α‐pyrones were developed according to substitution patterns target compounds. J. Heterocyclic Chem., (2011).
Promising multitargets ligands in Alzheimer's disease: sequential BuChE and DYRK1A/CLK1 kinases inhibition.
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...
The norepinephrine transporter (NET) plays an important role in neurotransmission and is involved a multitude of psychiatric neurodegenerative diseases. [123I/131I]meta-iodobenzylguanidine (MIBG) widely used radiotracer the diagnosis follow-up peripheral neuroendocrine tumors overexpressing transporter. MIBG does not cross blood–brain barrier (BBB), we have demonstrated "proof-of-concept" that 1,4-dihydroquinoline/quinolinium salt as chemical delivery system (CDS) promising tool to deliver...
The development of delivery systems to transport some specific radiotracers across the blood-brain barrier (BBB) needs be investigated for brain imaging. [18F]FLT (3'-deoxy-3'-18F-fluoro-l-thymidine), an analogue substrate nucleoside thymidine, has been developed as a proliferation tracer oncological PET studies. Unfortunately, low-grade tumors are poorly visualized due low uptake in tissue, preventing its use imaging detect at early stage. Based on our previous work, redox chemical system...
Abstract magnified image The synthesis and stereochemistry of a series new cyclic disulfides containing (poly)spirane 1,2‐dithiolane units are reported. Also included is study the self‐assembled monolayers ( SAMs ) these compounds on gold surface. characteristics resultant were determined by IR spectroscopy using molecular mechanics calculations.
The synthesis of some new compounds exhibiting two 1,3-perhydrooxazine units connected to the same aromatic ring and their ditosylated derivatives was carried out in good yields by direct condensation reaction corresponding aminoalcohols with dicarbonyl compounds. stereochemistry ring-chain tautomerism these were investigated NMR EI-MS. Keywords: 1,3-perhydrooxazine, tautomerism, conformational analysis, like-unlike isomers, NMR, massspectrometry
The DYRK (Dual-specificity tyrosine phosphorylation-regulated kinase) family of protein kinases is involved in the pathogenesis several neurodegenerative diseases. Among them, DYRK1A kinase thought to be implicated Alzheimer’s disease (AD) and Down syndrome, as such, has emerged an appealing therapeutic target. DYRKs are a subset CMGC (CDK, MAPKK, GSK3 CLK) group kinases. Within this kinases, CDC2-like (CLKs), such CLK1, closely related have also sparked great interest potential targets for...
Abstract The reaction is successfully applied in the synthesis of precursors known acetylcholinesterase inhibitors, e.
Abstract Review: 57 refs.
The title compound, C(21)H(17)ClO(3), which crystallizes as one of two possible oxo/hy-droxy-fulvene prototropic tautomers, possesses a strong intra-molecular O-H⋯O hydrogen bond that closes seven-membered ring. dihedral angles between the central five-membered ring and pendant rings are 55.05 (9) 44.51 (10)°. crystal packing is characterized by weak inter-molecular C-H⋯O inter-actions an H atom oxymethyl-ene unit carbonyl group adjacent mol-ecule, resulting in formation chains mol-ecules along axis.