A5103078517- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Biological Evaluation
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Synthesis and biological activity
- Cardiac Ischemia and Reperfusion
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Metabolomics and Mass Spectrometry Studies
- Neuroscience and Neuropharmacology Research
- Ion channel regulation and function
- Quinazolinone synthesis and applications
- Chemical Reaction Mechanisms
- Pancreatic function and diabetes
- Crystallography and molecular interactions
- Cancer, Hypoxia, and Metabolism
- Adenosine and Purinergic Signaling
- Synthesis and Reactions of Organic Compounds
- Chemical Reactions and Mechanisms
- Analytical Chemistry and Chromatography
- Synthesis of Organic Compounds
- Histone Deacetylase Inhibitors Research
- Synthesis and Reactivity of Heterocycles
- Synthesis of heterocyclic compounds
- Analytical Methods in Pharmaceuticals
University of Liège
2015-2024
Centre for Interdisciplinary Research in Rehabilitation
2022
Joint Research Center
2020
Istituto di Fisiologia Clinica
2015
University of Bologna
2015
Weatherford College
2007
Laboratoire de Chimie
2001-2007
Université Libre de Bruxelles
1996-2006
Novo Nordisk (United Kingdom)
2003
Institut Jacques Monod
1996
Gut microbiota may influence blood pressure (BP), namely via end products of carbohydrate fermentation. After informed consent, male volunteers were prospectively categorized into 3 groups upon European Society Hypertension criteria based on 24-hour ambulatory BP measurements: (1) hypertension, (2) borderline and (3) normotension. Stool, urine serum samples collected in fasting conditions. was characterized by 16S amplicon sequencing. Metabolomics, including quantification short-chain fatty...
Our study investigates the biochemical and functional impact of selective histone deacetylase 6 (HDAC6) inhibitors, a promising class novel therapeutics, in several cancer models. Selective HDAC6 inhibitors (Tubathian A, Tubastatin Tubacin Ricolinostat) non‐selective HDAC inhibitor (Vorinostat) were evaluated on cell lines derived from multiple tumour types both an vitro vivo setting as potential therapeutics. resulted α‐tubulin acetylation with no but failed to show any anti‐cancer...
Abstract Spheroids are three-dimensional cellular models with widespread basic and translational application across academia industry. However, methodological transparency guidelines for spheroid research have not yet been established. The MISpheroID Consortium developed a crowdsourcing knowledgebase that assembles the experimental parameters of 3,058 published spheroid-related experiments. Interrogation this identified heterogeneity in setup spheroids. Empirical evaluation interlaboratory...
The controlled polymerization of vinyl acetate has been recently achieved by several techniques, but PVAc with targeted Mn and low dispersity up to very high monomer conversions degrees was only obtained Co(acac)2 as controlling agent in the so-called CMRP, a type organometallic mediated radical (OMRP). Other techniques (including ATRP, ITP, TERP, RAFT/MADIX) have shown more or less pronounced slowdown kinetics, which attributed higher strength C–X bond between chain trapping (X) dormant...
A series of esters and amides 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid were synthesized evaluated in vitro for their inhibitory activity toward bovine α-chymotrypsin human leukocyte elastase. Both behaved as time-dependent inhibitors α-chymotrypsin, but ester-type coumarins clearly more efficient than the corresponding inactivating serine proteinase. The best inactivations observed with "aromatic" esters, particular meta-substituted phenyl such m-chlorophenyl...
"Omics" sciences have been developed to provide a holistic point of view biology and better understand the complexity an organism as whole. These systems approaches can be examined at different levels, starting from most fundamental, i.e., genome, finishing with functional, metabolome. Similar how genomics is applied exploration DNA, metabolomics qualitative quantitative study metabolites. This emerging field clearly linked genomics, transcriptomics, proteomics. In addition, provides unique...
A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators AMPA receptors. Attention was paid to the impact substituent introduced at 7-position heterocycle. The biological evaluation achieved by measuring current in rat cortex mRNA-injected Xenopus oocytes. most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (12a) found be active an object recognition test rats demonstrating cognition enhancing...
Ischemia/reperfusion (I/R) is the most common cause of acute kidney injury (AKI). Its pathophysiology remains unclear. Metabolomics dedicated to identify metabolites involved in (patho)physiological changes integrated living systems. Here, we performed 1H-Nuclear Magnetic Resonance metabolomics using urine, serum and samples from a mouse model renal I/R.Renal 30-min ischemia was induced 12-week-old C57BL/6J male mice by bilaterally clamping vascular pedicles, followed 6, 24 or 48-hour...
We report here the synthesis of 7-phenoxy-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides and their evaluation as AMPA receptor positive allosteric modulators (AMPApams). The impact substitution on phenoxy ring nitrogen atom at 4-position was examined. At GluA2(Q) expressed in HEK293 cells (calcium flux experiment), most potent compound 11m (4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, EC50 = 2.0 nM). Hill coefficient screening shape...
Abstract Kidney injury is a common complication of severe disease. Here, we report that injuries the zebrafish embryonal kidney are rapidly repaired by migratory response in 2-, but not 1-day-old embryos. Gene expression profiles between these two developmental stages identify cxcl12a and myca as candidates involved repair process. Zebrafish embryos with , cxcr4b or deficiency display abnormalities, confirming their role to injury. In mice kidney-specific knockout, Cxcl12 Myc gene deletions...
In the search of a potent cognitive enhancer, series 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators AMPA receptors. present work, we focused our efforts on insertion mono- or polyfluoro-substituted alkyl chains at 4-position thiadiazine ring in an attempt to enhance pharmacokinetic behavior previously described compounds. Among all compounds, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide,...
A series of 4H-1,2,4-pyridothiadiazine 1,1-dioxides and 2, 3-dihydro-4H-1,2,4-pyridothiadiazine bearing various alkyl aryl substituents on the 2-, 3-, 4-positions was synthesized tested as possible positive allosteric modulators (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors. Many compounds were found to be more potent than reference diazoxide aniracetam potentiators AMPA current in rat cortex mRNA-injected Xenopus oocytes. The most active compound,...
4-N-Subsituted and -unsubstituted 3-alkyl- 3-(alkylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides were synthesized tested vs diazoxide selected 3-(alkylamino)-7-chloro-4H-1,2,4-benzothiadiazine as potassium channel openers on pancreatic vascular tissues. Several 4-N-unsubstituted 3-(alkylamino)pyridothiadiazines some 3-(alkylamino)-7-chlorobenzothiadiazines found to be more potent than for the inhibition of insulin-releasing process. Moreover, appeared selective tissue. By means...
3-(Alkylamino)-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides were synthesized, and their activity on rat-insulin-secreting cells rat aorta rings was compared to that of the KATP channel activators diazoxide pinacidil. Structure−activity relationships indicated an improved potency selectivity for pancreatic tissue obtained by introducing a fluorine atom in 7-position short linear (preferably ethyl) or cyclic cyclobutyl) hydrocarbon chain nitrogen 3-position. By contrast, strong myorelaxant...
The present work explored 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides diversely substituted in the 7-position. Those compounds, structurally related to previously described potassium channel openers such as benzothiadiazine dioxide BPDZ 73, were tested putative KATP activators on pancreatic endocrine tissue and vascular smooth muscle tissue. nature of substituent introduced 7-position well alkylamino side chain 3-position strongly affected both potency selectivity...
ABSTRACT Introduction As a complement to the classic metabolomics biofluid studies, visualisation of metabolites contained in cells or tissues could be very powerful tool understand how local metabolism and biochemical pathways affected by external internal stimuli pathologies. Therefore, extraction and/or lysis is necessary obtain samples adapted for use with current analytical tools (liquid NMR MS). These work‐ups are often most labour‐intensive rate‐limiting steps metabolomics, as they...