Search results for "Sulfone"

showing 10 items of 113 documents

Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

2019

This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...

Trypanosoma brucei rhodesienseStrong inhibitorKetoneStereochemistryProtein ConformationPeptide01 natural sciences03 medical and health sciencesStructure-Activity RelationshipSUBSTRATEDrug DiscoverymedicineHumansAfrican trypanosomiasisSulfonesBIOLOGICAL EVALUATION030304 developmental biologyWARHEADchemistry.chemical_classification0303 health sciencesMolecular StructureChemistryDERIVATIVESTrypanosoma brucei rhodesienseCYSTEINE PROTEASES RHODESAIN BIOLOGICAL EVALUATION CATHEPSIN-L INHIBITORS BRUCEI PEPTIDOMIMETICS FALCIPAIN-2 DERIVATIVES SUBSTRATE WARHEADBRUCEImedicine.diseaseFALCIPAIN-2Trypanocidal Agents0104 chemical sciences010404 medicinal & biomolecular chemistryCysteine EndopeptidasesTrypanosomiasis AfricanCYSTEINE PROTEASES RHODESAINCATHEPSIN-LMolecular MedicineINHIBITORSPEPTIDOMIMETICS
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Copper-catalyzed regioselective synthesis of (E)-β-fluorovinyl sulfones

2019

Organofluorine compounds are finding increasing application in a variety of fields such as pharmaceutical, agrochemical, and material sciences. However, given the scarcity of fluorine-containing natural products, advancement in this area depends almost entirely on the development of new synthetic methodologies. In this article, we present the synthesis of a series of previously undescribed (E)-&beta

Vinyl CompoundsPharmaceutical Sciencealkynyl sulfonesChemical synthesisArticleCatalysisAnalytical ChemistrySulfonelcsh:QD241-441chemistry.chemical_compoundlcsh:Organic chemistryorganofluorine chemistryDrug DiscoveryOrganic chemistryPhysical and Theoretical Chemistrycopper catalysisMolecular StructureOrganic ChemistryRegioselectivityFluorineHydrogen fluorideOrganofluorine chemistryβ-fluorovinyl sulfonechemistryChemistry (miscellaneous)regioselectivityCopper catalyzedMolecular MedicineOrganofluorine compoundshydrogenationCopper
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Synthesis, stability and spectral behavior of fluorogenic sulfone-pyronin and sulfone-rosamine dyes

2018

International audience; The first synthesis of sulfone-pyronin and sulfone-rosamine dyes bearing optically tunable primary amino groups (acting as fluorogenic centers) is presented. Sulfone analogs of xanthene-based fluorophores have recently been highlighted as a new class of near-infrared (NIR) fluorescent dyes (Liu et al. ACS Appl Mater Interfaces 2016; 8(35):22953-62), and the availability of fluorogenic derivatives is essential for the rapid construction of “turn-on” reactive probes for chemoselective bioimaging. However, these fluorescent anilines have been found to be unstable in aqueous physiological conditions due to the marked electrophilicity of their meso-position and hence its …

XantheneAqueous solutionPrimary (chemistry)NIR dye010405 organic chemistryHetero-xanthene dye[CHIM.ORGA]Chemical Sciences/Organic chemistryProcess Chemistry and TechnologyGeneral Chemical EngineeringFluorogenic enzyme substrateRosamine010402 general chemistry01 natural sciencesFluorescenceCombinatorial chemistry0104 chemical sciencesSulfonechemistry.chemical_compoundNucleophilechemistryElectrophileMoleculePyronin
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Sildenafil protects epithelial cell through the inhibition of xanthine oxidase and the impairment of ROS production

2009

Recent reports suggest that xanthine oxidase (XO), a modified form of the native xanthine dehydrogenase enzyme, plays an important role in various forms of ischemic and vascular injuries, inflammatory diseases, and chronic heart failure. The XO inhibitors allopurinol and its oxidation product oxypurinol held considerable promises in the treatment of these conditions both in experimental animals and in human clinical trials. More recently, an endothelium-based protective effect of sildenafil, a well-known type-5 phosphodiesterase inhibitor, has been reported in preconditioning prior to ischemia/reperfusion in healthy human subjects. Based on the structural similarities between allopurinol an…

Xanthine OxidasePurinonesEndotheliumCell SurvivalSildenafilIschemiaAllopurinolPharmacologyBiochemistryPiperazinesSildenafil CitrateStructure-Activity Relationshipchemistry.chemical_compoundSettore BIO/10 - BiochimicaTumor Cells CulturedmedicineHumansSulfonesXanthine oxidaseNADPH oxidasebiologybusiness.industryEpithelial CellsGeneral Medicinemedicine.diseasemedicine.anatomical_structurechemistryBiochemistryPurinesCell cultureSettore BIO/14 - Farmacologiabiology.proteinReactive Oxygen SpeciesZaprinastbusinessXanthine oxidase ROS production oxidative stress inhibition sildenafil zaprinast human mammary epithelial cellsmedicine.drugFree Radical Research
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Chemoselektive Fluoreszenzstudien am Subtilisin und “Thiosubtilisin”

1985

Chemoselective Fluorescence Studies with Subtilisin and “Thiosubtilisin” The serine hydroxy group in the active site of subtilisin is selectively “phosphylated”3). This is demonstrated using the fluorescent phosphinic fluoride 1. “Thiosubtilisin” does not react with 1 but with the SH-selective and fluorescent vinyl sulfone 2.

biologyStereochemistryfungiOrganic ChemistryHydroxy groupSubtilisinActive siteVinyl sulfoneFluorescenceSerineenzymes and coenzymes (carbohydrates)chemistry.chemical_compoundchemistrybiology.proteinOrganic chemistryPhysical and Theoretical ChemistryFluorideLiebigs Annalen der Chemie
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Palladium-catalyzed heteroaryl thioethers synthesis overcoming palladium dithiolate resting states inertness: Practical road to sulfones and NH-sulfo…

2018

International audience; We provide efficient synthetic access to heteroaryl sulfones in two-steps using a simple palladium-1,1'-bis [(diphenyl)phosphanyl]ferrocene catalyst to form in high yields variously functionalized heteroaromatic thioethers. Pyridinyl-containing substrates can be subsequently selectively oxidized into sulfones and NH-sulfoximines by using very mild oxidation conditions with a high functional group tolerance. In the palladium catalyzed C-S coupling of heteroaromatic thiols, reactivity limitation is attached with electron-deficient thiols. We show that this limitation can be resolved by the successful use of 2-bromoheteroarenes in the C-S coupling. We established herein…

bond formationarenessulfideschemistry.chemical_element010402 general chemistry01 natural sciencesCatalysisefficientCatalysischemistry.chemical_compounds-arylation[CHIM]Chemical SciencesReactivity (chemistry)SulfonesResting statethiols[PHYS]Physics [physics]010405 organic chemistryProcess Chemistry and TechnologyGeneral Chemistryindolesacid saltsCombinatorial chemistry0104 chemical sciencesThiolatesC-S couplingchemistryFerroceneNH-sulfoximinesReagentElectrophileFunctional groupH functionalizationdirecting groupPalladiumStoichiometryPalladiumCatalysis Communications
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Solid state electrochemical behavior of organosulfur compounds

2017

Abstract The solid-sate electrochemistry of organosulfur compounds existing in petroleum and its derived matrices is described using the voltammetry of immobilized microparticles methodology. Cyclic and square wave voltammogrammetric responses of sulfur compounds responsible of aging of asphalt pavements, namely, thiophenes, disulfides, sulfides, sulfoxides and sulfones were determined at compound-modified graphite electrodes in contact with 0.10 M H2SO4. The electrochemical oxidation/reduction products were characterized by attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) and scanning electron microscopy with energy dispersion x-ray detection (SEM-EDX) couple…

chemistry.chemical_classificationChemistryGeneral Chemical Engineering010401 analytical chemistryInorganic chemistrychemistry.chemical_element02 engineering and technologySulfonic acid021001 nanoscience & nanotechnologyElectrochemistry01 natural sciencesSulfur0104 chemical sciencesAnalytical ChemistrySulfonechemistry.chemical_compoundAttenuated total reflectionElectrochemistryFourier transform infrared spectroscopy0210 nano-technologyDissolutionOrganosulfur compoundsJournal of Electroanalytical Chemistry
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Environmental analysis of chlorinated aromatic thioethers, sulphoxides and sulphones

1993

Abstract Chlorinated aromatic thioethers discussed here are polychlorinated dibenzothiophenes, thianthrenes and diphenylsulphides. Relatively little is known about their occurrence, behaviour and fate in the environment. Polychlorinated dibenzothiophenes and diphenylsulphides have recently been found to be formed in waste combustion and analysed in pulp mill effluents. Chlorinated sulphoxides and sulphones are usually metabolites or oxidation products of different chlorinated aromatic compounds. Different gas chromatographic-mass spectrometric techniques are used in the analysis of the chlorinated thioethers. The sulphoxides and sulphones, because of their higher polarity, can be isolated f…

chemistry.chemical_classificationChromatographyEnvironmental analysisOrganic ChemistrySulfoxideGeneral MedicineBiochemistryHigh-performance liquid chromatographyThin-layer chromatographyAnalytical ChemistrySulfonechemistry.chemical_compoundchemistrypolycyclic compoundsThiolOrganic chemistryGas chromatographyWaste combustionJournal of Chromatography A
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New acetylenes fromChrysanthemum coronarium L.

1990

The investigation of the aerial parts of Chrysanthemum coronarium yielded, in addition to several known compounds, two new acetylenic sulfoxides 9 and 10, and a new thiophene spiroacetal enol ether 11. Their structures were deduced by spectroscopic and chemical methods.

chemistry.chemical_classificationChrysanthemum coronariumStereochemistryOrganic ChemistrySulfoxideNuclear magnetic resonance spectroscopySulfonechemistry.chemical_compoundchemistryEnol etherThiopheneOrganic chemistryMoleculePhysical and Theoretical ChemistryLiebigs Annalen der Chemie
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Quick and reliable routes to phase diagrams for polyethersulfone and polysulfone membrane formation

2000

Phase diagrams were measured and calculated for the ternary membrane forming systems DMF/water/polysulfone and DMF/water/polyethersulfone at different temperatures. Customary experiments yielded cloud point curves, tie lines, and critical compositions. The theoretical computation starts from the Flory-Huggins theory and employs binary interaction parameters g ij that vary with the composition. This information was mainly obtained by means of Headspace-Gas Chromatography (HSGC, yielding the partial pressures of the volatile components); these data were complemented by light scattering and swelling experiments. The calculation of binodals, spinodals, tie lines, and critical points avoids the …

chemistry.chemical_classificationCloud pointPolymers and PlasticsOrganic ChemistryPolymerFlory–Huggins solution theoryCondensed Matter PhysicsLight scatteringGibbs free energychemistry.chemical_compoundsymbols.namesakechemistryPolymer chemistryMaterials ChemistrysymbolsPolysulfonePhysical and Theoretical ChemistryTernary operationPhase diagramMacromolecular Chemistry and Physics
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