Search results for "steric"

showing 10 items of 476 documents

Preparation, Properties, and Reactivity of (Aminoferrocenyl)(ferrocenyl)carbene(pentacarbonyl)chromium(0) as Bulky Isolobal Trimetallo-amide

2015

Nucleophilic substitution of the ethoxy substituent in the Fischer carbene complex (ethoxy)(ferrocenyl)carbene(pentacarbonyl)chromium(0) (1) by ferrocenyl amide [Fc-NH]– [2-H]– gives the hetero trimetallic complex (aminoferrocenyl)(ferrocenyl)carbene (pentacarbonyl)chromium(0) (3). As the Cr(CO)5 fragment is isolobal to oxygen or sulfur 3 can be viewed as an isolobal metallo analogue to diferrocenylamide (Fc)(FcNH)C=O (4) and diferrocenylthioamide (Fc)(FcNH)C=S (5). The impact of the formal replacement of O/S by Cr(CO)5 in 3 is studied with respect to steric and electronic consequences as well as reactivity by spectroscopic, diffraction, electrochemical and theoretical methods.

Inorganic ChemistrySteric effectschemistry.chemical_compoundchemistryFerroceneAmideTransition metal carbene complexNucleophilic substitutionOrganic chemistryReactivity (chemistry)Isolobal principleMedicinal chemistryCarbeneZeitschrift für anorganische und allgemeine Chemie
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Investigation of the Enantioselectivity Observed in Epoxidation Reactions Catalysed by Bis‐Strapped Chiral Porphyrins Derived from L ‐Proline

2002

The enantiomeric excesses obtained during the epoxidation reactions of p-chlorostyrene or 1,2-dihydronaphthalene catalysed by two different series of chiral porphyrins are reported. An attempt is made to correlate the enantioselectivity with the steric hindrance generated by the straps of these catalysts. It is shown that this steric hindrance is influenced by the nature of the strap and that it can be approximated. Additionally, the same strap is tethered in two different fashions on each side of the porphyrin, leading to either D2- or C2-symmetrical catalysts, for which the two sides are identically functionalised.

Inorganic ChemistrySteric effectschemistry.chemical_compoundchemistryOrganic chemistryProlineEnantiomerMedicinal chemistryPorphyrinCatalysisEuropean Journal of Inorganic Chemistry
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Mass Spectrometric Investigation of Noncovalent Complexation between a Tetratosylated Resorcarene and Alkyl Ammonium Ions

2004

Noncovalent complexation between tetratosylated tetraethyl resorcarene (1) and primary, secondary, and tertiary alkyl ammonium ions (mMe, dMe, tMe, mEt, dEt, tEt, dBu, and dHex) was studied by electrospray ionization Fourier transform ion cyclotron resonance (ESI-FTICR) mass spectrometry. Interactions of the noncovalent complexes were investigated by means of competition experiments, collision-induced dissociation (CID) experiments, ion-molecule reactions with tripropylamine and gas phase H/D-exchange reactions with deuteroammonia. Gas phase ion-molecule reactions gave especially valuable information about the structure and properties of the complexes. Resorcarene 1 formed relatively stable…

IonsSteric effectschemistry.chemical_classificationSpectrometry Mass Electrospray IonizationMolecular StructureMacromolecular SubstancesChemistryHydrogen bondOrganic ChemistryInorganic chemistryGeneral ChemistryCatalysisDissociation (chemistry)Fourier transform ion cyclotron resonanceQuaternary Ammonium CompoundsTosyl Compoundschemistry.chemical_compoundPolymer chemistryProton affinityNon-covalent interactionsAmmoniumAlkylChemistry - A European Journal
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Control of the spin state by charge and ligand substitution: two-step spin crossover behaviour in a novel neutral iron(II) complex

2014

The influence of the charge and steric hindrance on the spin state of a series of four monomeric Fe-II complexes derived from the tridentate tigands 2-(1H-benzoimidazol-2-yl)-1,10-phenanthroline (Hphenbi) and 2-(1H-benzoimidazol-2-yl-9-methyl-1,10-phenanthroline (Hmphenbi) and their deprotonated forms (phenbi(-), mphenbi(-)) are investigated. The crystal structure and magnetic properties show that [Fe(Hphenbi)(2)](BF4)(2)center dot 1.5C(6)H(5)NO(2)center dot H2O (1) and its neutral form [Fe(phenbi)(2)]center dot 2CHCl(3)center dot H2O (2) are low-spin complexes at 400 K due to the strong ligand field imparted by the terpyridine-like tigand. In contrast, the steric hindrance induced by the m…

Ligand field theorySteric effectsSpin statesChemistryStereochemistryLigandHydrostatic pressureCrystal structureInorganic ChemistrySpin crossoversCrystallographyDeprotonationSpin crossoverFISICA APLICADALigand substitutionSpin stateIron complex
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Supramolecular Spintronic Devices: Spin Transitions and Magnetostructural Correlations in[Fe4IIL4]8+[2×2]-Grid-Type Complexes

2003

The magnetism of a series of tetranuclear complexes of the [Fe4IIL4]8+ [2x2]-grid-type was investigated, revealing the occurrence of spin transition behavior within this class of compounds. The phenomenon depends directly on the nature of the substituent R(1) in the 2-position on the central pyrimidine group of the ligand L. All Fe(II) ions in compounds with R(1) substituents favoring strong ligand fields (R(1)=H; OH) remain completely in the diamagnetic low-spin state. Only complexes bearing R(1) substituents attenuating the ligand field by steric (and to a lesser extent electronic) effects (R(1)=Me; Ph) exhibit spin transition behavior triggered by temperature. In general, gradual and inc…

Ligand field theorySteric effectsSpintronicsStereochemistryMagnetismLigandChemistryOrganic ChemistrySpin transitionSupramolecular chemistryGeneral ChemistryCatalysisCrystallographySpin (physics)Chemistry - A European Journal
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Multiple actions of fenamates and other nonsteroidal anti-inflammatory drugs on GABAA receptors

2019

The nonsteroidal anti-inflammatory drug (NSAID) niflumic acid, a fenamate in structure, has many molecular targets, one of them being specific subtypes of the main inhibitory ligand-gated anion channel, the GABA(A) receptor. Here, we report on the effects of other fenamates and other classes of NSAIDs on brain picrotoxinin-sensitive GABA A receptors, using an autoradiographic assay with [S-35]TBPS as a ligand on mouse brain sections. We found that the other fenamates studied (flufenamic acid, meclofenamic acid, mefenamic acid and tolfenamic acid) affected the autoradiographic signal at low micromolar concentrations in a facilitatory-like allosteric fashion, i.e., without having affinity to …

MECHANISM0301 basic medicineNSAID drugsMefenamic acidAllosteric regulationPharmacologyBINDING-SITESGABA03 medical and health sciences0302 clinical medicineTolfenamic acidNiflumic acidmedicineSHIFTMODULATIONReceptorXenopus oocytesAGENTPharmacologyChemistryGABAA receptorNiflumic acidANION GRADIENTA RECEPTORSSUBUNITS3. Good healthMeclofenamic acidFenamates030104 developmental biologyFlufenamic acid317 PharmacyACIDAutoradiography030217 neurology & neurosurgeryRecombinant GABA(A) receptorsRESPONSESmedicine.drugEuropean Journal of Pharmacology
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Decoding the Folding of Burkholderia glumae Lipase: Folding Intermediates En Route to Kinetic Stability

2012

The lipase produced by Burkholderia glumae folds spontaneously into an inactive near-native state and requires a periplasmic chaperone to reach its final active and secretion-competent fold. The B. glumae lipase-specific foldase (Lif) is classified as a member of the steric-chaperone family of which the propeptides of alpha-lytic protease and subtilisin are the best known representatives. Steric chaperones play a key role in conferring kinetic stability to proteins. However, until present there was no solid experimental evidence that Lif-dependent lipases are kinetically trapped enzymes. By combining thermal denaturation studies with proteolytic resistance experiments and the description of…

Macromolecular AssembliesProtein StructureProtein FoldingBurkholderiaProtein ConformationStereochemistryBiophysicslcsh:MedicineBiochemistryProtein Chemistrybacterial lipasemolten globuleBacterial ProteinsNative stateBurkholderia glumaeLipaseProtein Interactionslcsh:ScienceBiologyMultidisciplinarybiologylipase-specific foldasePhysicslcsh:RSubtilisinProteinsLipasebiology.organism_classificationMolten globuleEnzymesChaperone ProteinsKineticsBiochemistryChaperone (protein)Enzyme StructureProteolysisFoldasebiology.proteinlcsh:Qsteric chaperoneProtein foldingnear-native folding intermediateResearch ArticleMolecular Chaperones
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Cooperative Transition in the Conformation of 24-Mer Tarantula Hemocyanin upon Oxygen Binding

2005

Hemocyanins are large respiratory proteins of arthropods and mollusks, which bind oxygen with very high cooperativity. Here, we investigated the relationship between oxygen binding and structural changes of the 24-mer tarantula hemocyanin. Oxygen binding of the hemocyanin was detected following the fluorescence intensity of the intrinsic tryptophans. Under the same conditions, structural changes were monitored by the non-covalently bound fluorescence probe Prodan (6-propionyl-2-(dimethylamino)-naphthalene), which is very sensitive to its surroundings. Upon oxygen binding of the hemocyanin a red shift of 5 nm in the emission maximum of the label was observed. A comparison of oxygen binding c…

Macromolecular SubstancesProtein ConformationPartial Pressuremedicine.medical_treatmentAllosteric regulationMolecular ConformationAnalytical chemistrychemistry.chemical_elementchemical and pharmacologic phenomenaCooperativitycomplex mixturesBiochemistryOxygenProtein structure2-NaphthylaminemedicineAnimalsBinding siteMolecular BiologyBinding SitesChemistryTryptophanSpidersHemocyaninCell BiologyFluorescenceOxygenSpectrometry FluorescenceMicroscopy FluorescenceModels ChemicalSpectrophotometryHemocyaninsBiophysicsAllosteric SiteOxygen bindingProtein BindingJournal of Biological Chemistry
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Neuroprotective action of diazepam at very low and moderate doses in Alzheimer's disease model rats

2018

Abstract Early manifestations of Alzheimer's disease (AD) include neuroinflammation, disrupted neurotransmission and cognitive deficits. Impairment of the GABAergic system is essentially involved in the pathogenesis of AD. Traditionally, agonists of GABAA receptors at doses above 1 mg/kg are known to possess memory impairing effects. However, we have previously found that GABAA receptor GABA site ligand muscimol at very low doses acted contrary – enhanced spatial learning/memory, as well as prevented neuroinflammation and augmented neurotransmission in AD model rats. Therefore, in the present study we focused on the assessment of the effects of non-sedative – very low (0.05 mg/kg) and moder…

Male0301 basic medicineAllosteric modulatormedicine.drug_classSynaptophysinNeurotransmissionPharmacologyHippocampusNeuroprotectionRandom Allocation03 medical and health sciencesCellular and Molecular Neurosciencechemistry.chemical_compound0302 clinical medicineAlzheimer DiseasemedicineAnimalsGliosisRats Wistargamma-Aminobutyric AcidCerebral CortexPharmacologyMemory DisordersBenzodiazepineDiazepamDose-Response Relationship DrugGlutamate DecarboxylaseGABAA receptorAcetylcholineNeuroprotective Agents030104 developmental biologyGene Expression RegulationMuscimolchemistryAstrocytesSynaptic plasticityGABAergic030217 neurology & neurosurgeryNeuropharmacology
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Novel Analgesic Agents Obtained by Molecular Hybridization of Orthosteric and Allosteric Ligands

2019

AbstractDespite the high incidence of acute and chronic pain in the general population, the efficacy of currently available medications is unsatisfactory. Insufficient management of pain has a profound impact on the quality of life and can have serious physical, psychological, social, and economic consequences. This unmet need reflects a failure to develop novel classes of analgesic drugs with superior clinical properties and lower risk of abuse. Nevertheless, recent advances in our understanding of the neurobiology of pain are offering new opportunities for developing different therapeutic approaches. Among those, the activation of M2 muscarinic acetylcholine receptors, which play a key ro…

Male0301 basic medicineGuinea PigsPopulationAnalgesicAllosteric regulationPainIn Vitro TechniquesMotor ActivityLigandsBioinformaticsAnalgesic agentsMice03 medical and health sciences0302 clinical medicineAllosteric RegulationDrug DiscoveryMuscarinic acetylcholine receptormedicineAnimalsHeart AtriaeducationPharmacologyAnalgesicsReceptor Muscarinic M2education.field_of_studyBehavior AnimalDose-Response Relationship Drugbusiness.industryChronic painmedicine.diseaseMolecular hybridization030104 developmental biologyTolerabilityCholinergicAtrial Function LeftbusinessAllosteric Site030217 neurology & neurosurgery
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