Search results for "Valuation"

showing 10 items of 2494 documents

Single-dose ebselen does not afford sustained neuroprotection to rats subjected to severe focal cerebral ischemia

2004

Oxygen free radicals have been involved in the pathophysiology of cerebral ischemia, especially after spontaneous or thrombolytic reperfusion. In this study with rats, we have combined a severe focal ischemic insult (2 h) and a prolonged reperfusion time (7 days) to assess the possible sustained neuroprotective effect of ebselen (10 or 100 mg/kg), a small, lipophilic organoselenium compound which mimics glutathione peroxidase. Parietal cortical perfusion was measured by laser-Doppler flowmetry, and focal cerebral ischemia was carried out by the intraluminal thread method. We have measured plasma selenium levels, brain reduced glutathione levels, as a marker of oxidative stress, and infarct …

AzolesMaleTime FactorsCentral nervous systemDrug Evaluation PreclinicalIschemiaAdministration OralIsoindolesPharmacologymedicine.disease_causeNeuroprotectionDrug Administration ScheduleBrain IschemiaSeleniumchemistry.chemical_compoundOrganoselenium CompoundsAnimalsMedicineRats WistarBrain ChemistryPharmacologychemistry.chemical_classificationbusiness.industryEbselenCerebral infarctionGlutathione peroxidaseBody WeightBrainInfarction Middle Cerebral ArteryGlutathionemedicine.diseaseGlutathioneRatsOxidative Stressmedicine.anatomical_structurechemistrySpainAnesthesiaReperfusionReactive Oxygen SpeciesbusinessOxidative stressEuropean Journal of Pharmacology
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Discovery of 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles as potent firefly luciferase inhibitors.

2013

Luciferase reporter assays are commonly used in high-throughput screening methods. Here, we report new firefly luciferase (FLuc) inhibitors based on 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles, which showed up as "false positives" in a luciferase reporter gene-based assay for nuclear receptor antagonists. The inhibition was shown to be noncompetitive for both natural enzyme substrates (d-luciferin and ATP) and selective to FLuc and proven to arise from a direct interaction between the enzyme and the inhibitor. Of the 63 evaluated compounds, 28 showed significantly better inhibition potency than the well-known inhibitor resveratrol (IC(50) = 59 nM), with fi…

AzolesModels MolecularMagnetic Resonance SpectroscopyStereochemistryDrug Evaluation PreclinicalResveratrolCell Linechemistry.chemical_compoundInhibitory Concentration 50Drug DiscoveryScreening methodIc50 valuesPotencyAnimalsLuciferaseEnzyme InhibitorsLuciferasesIC50ta116chemistry.chemical_classificationFirefliesEnzymechemistryNuclear receptorBiochemistryMolecular MedicineJournal of medicinal chemistry
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Solution versus Fluorous versus Solid-Phase Synthesis of 2,5-Disubstituted 1,3-Azoles. Preliminary Antibacterial Activity Studies

2009

A small library of compounds with an oxa(thia)zole scaffold and structural diversity in both positions 2 and 5 has been synthesized. Double acylation of a protected glycine affords intermediate α-amido-β-ketoesters, which in turn can be dehydrated to afford 1,3-oxazoles or reacted with Lawesson’s reagent to furnish 1,3-thiazoles. This procedure was designed with its adaptation to fluorous techniques in mind. Thus, when a protected glycine with a fluorous tag in the ester moiety is used as a starting material, the synthesis can be easily completed without column chromatography purification of intermediate compounds with good to excellent yields, thus affording a suitable entry to the prepara…

AzolesStaphylococcus aureusANTIBACTERIAL ACTIVITYDrug Evaluation PreclinicalMicrobial Sensitivity TestsChemical synthesisSmall Molecule LibrariesAcylationchemistry.chemical_compoundSolid-phase synthesisColumn chromatographyAZOLESOrganic chemistryMoietyAntibacterial agentChemistryOrganic ChemistryCiencias QuímicasFLUOROUSCombinatorial chemistryAnti-Bacterial AgentsSolutionsQuímica OrgánicaMolecular ProbesSOLID-PHASELawesson's reagentAntibacterial activityCIENCIAS NATURALES Y EXACTAS
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DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL HETEROCYCLIC DERIVATIVES AS MODULATORS OF B-DNA AND G-QUADRUPLEXES DNA FUNCTIONS

B-DNA G-QUADRUPLEXES (G4s) HETEROCYCLIC DERIVATIVES DESIGN SYNTHESIS BIOLOGICAL EVALUATION
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Operator splitting methods for American option pricing

2004

Abstract We propose operator splitting methods for solving the linear complementarity problems arising from the pricing of American options. The space discretization of the underlying Black-Scholes Scholes equation is done using a central finite-difference scheme. The time discretization as well as the operator splittings are based on the Crank-Nicolson method and the two-step backward differentiation formula. Numerical experiments show that the operator splitting methodology is much more efficient than the projected SOR, while the accuracy of both methods are similar.

Backward differentiation formulaMathematical optimizationPartial differential equationDiscretizationApplied MathematicsFinite difference methodSemi-elliptic operatorTime discretizationValuation of optionsComplementarity theoryLinear complementarity problemCrank–Nicolson methodOperator splitting methodAmerican optionMathematicsApplied Mathematics Letters
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Physical exercise and prevention of falls. Effects of a Pilates training method compared with a general physical activity program

2021

Introduction Falls are the leading cause of injury-related mortality and morbidity in the elderly. Physical activity plays a key role in the prevention of falls and stimulates postural control. The aim of this study was to compare a general physical activity program for the elderly with a Pilates program to evaluate the effects on balance and on reducing the risk of falling. Materials and methods Forty-six subjects were enrolled in this study, but only 41 were included in the study. The subjects were divided into 2 groups: Pilates group (P-G) and a group following a nonspecific program of physical activity (Pa-G). Each subject underwent the hand grip test, Berg balance scale test, and postu…

BalanceMaleProgram evaluationmedicine.medical_specialtyPosturePhysical exerciselaw.invention03 medical and health sciences0302 clinical medicineRandomized controlled triallawHand strengthmedicinePostural BalanceHumansPhysical activity program030212 general & internal medicineExerciseGeriatric AssessmentPostural BalancePhysical Therapy ModalitiesAgedBalance (ability)Aged 80 and overHand Strengthbusiness.industryGeneral MedicineMiddle AgedTest (assessment)030220 oncology & carcinogenesisBerg Balance ScalePhysical therapyExercise Movement TechniquesFallsAccidental FallsFemalePilatesbusinessProgram EvaluationMedicine
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Battery characterization via eddy-current imaging with nitrogen-vacancy centers in diamond

2021

Sensitive and accurate diagnostic technologies with magnetic sensors are of great importance for identifying and localizing defects of rechargeable solid batteries in a noninvasive detection. We demonstrate a microwave-free AC magnetometry method with negatively charged NV centers in diamond based on a cross-relaxation feature between NV centers and individual substitutional nitrogen (P1) centers occurring at 51.2 mT. We apply the technique to non-destructive solid-state battery imaging. By detecting the eddy-current-induced magnetic field of the battery, we distinguish a defect on the external electrode and identify structural anomalies within the battery body. The achieved spatial resolut…

Battery (electricity)Materials scienceMagnetometerFOS: Physical sciences02 engineering and technologyApplied Physics (physics.app-ph)engineering.materiallcsh:Technology01 natural scienceslaw.inventionlcsh:ChemistrylawVacancy defecteddy current imaging0103 physical sciencesEddy currentGeneral Materials Science010306 general physicsNV-centers in diamondlcsh:QH301-705.5Instrumentationnondestructive evaluationFluid Flow and Transfer Processeslcsh:Tbusiness.industryProcess Chemistry and TechnologyGeneral EngineeringDiamond600Physics - Applied Physics021001 nanoscience & nanotechnologylcsh:QC1-999Computer Science ApplicationsMagnetic fieldlcsh:Biology (General)lcsh:QD1-999lcsh:TA1-2040Electrodebattery diagnosticsengineeringOptoelectronicslcsh:Engineering (General). Civil engineering (General)0210 nano-technologyAlternating currentbusinessddc:600lcsh:Physics
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Efficient contactless power transfer system for EVs

2016

Based on the inductive power transfer (IPT), the contactless approach allows safe and comfortable operations of battery charging for Electric Vehicles (EVs). In this paper, a contactless system particularly suitable for E-bike battery charging is proposed. A practical realization of the system has been carried out, aiming at the system evaluation in terms of working and efficiency. Through a phase shift modulation, a power regulation has been implemented. The target power level is 100 W.

Battery (electricity)Power regulationbusiness.industryComputer science020208 electrical & electronic engineeringelectric vehicleElectrical engineeringSystem evaluation02 engineering and technologySettore ING-IND/32 - Convertitori Macchine E Azionamenti ElettriciPower levelelectric vehicles; inductive power transfer; contactless charging; vehicle-to-grid.ModulationLogic gate0202 electrical engineering electronic engineering information engineeringcontactless chargingMaximum power transfer theoremComputerSystemsOrganization_SPECIAL-PURPOSEANDAPPLICATION-BASEDSYSTEMS020201 artificial intelligence & image processinginductive power transfervehicle-to-gridbusinessRealization (systems)electric vehicles
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Integrating the human factor in FMECA-based risk evaluation through Bayesian networks

2020

The contribution of the present paper aims to develop the traditional Failure Modes, Effects and Criticality Analysis (FMECA) for quantitative risk analysis from a Bayesian Network (BN)-based perspective. The main purpose of research consists in providing a framework for analysing causal relationships for risk evaluation and deriving probabilistic inference among significant risk factors. These parameters will be represented by linguistic variables and will include the human factor as a key element of analysis. Traditional approaches for risk evaluation and management performed by FMECA [1] represent helpful tools to globally enhance systems and processes conditions [2]. However, such appro…

Bayesian NetworkSettore ING-IND/17 - Impianti Industriali MeccaniciHuman FactorRisk evaluationMATEMATICA APLICADAFMECA
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Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis

2018

Abstract: Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence, there is a need to identify new molecular scaffolds and targets as potential therapeutics for the treatment of this disease. We report a small series of 1,2‐substituted‐1H‐benzo[d]imidazole derivatives (9ad) showing affinity in the submicromolar range (Ki = 0.150.69 μM) toward Leishmania mexicanaCPB2.8ΔCTE, one of the more promising targets for antileishmanial drug design. The compounds confirmed activity in vitro against intrace…

BenzimidazoleCell SurvivalIn silicoLeishmania mexicanaAntiprotozoal AgentsDrug Evaluation PreclinicalProtozoan ProteinsDrug resistanceCysteine Proteinase InhibitorsPharmacologyAntileishmanial agents Benzimidazole derivatives Docking studies In silico profiling Leishmania mexicanaCPB2.8 Biochemistry Molecular Medicine01 natural sciencesBiochemistryLeishmania mexicanaCell LineInhibitory Concentration 50chemistry.chemical_compoundCysteine ProteasesDrug DiscoverymedicineHumansAmastigoteLeishmaniasisBiologyEnzyme AssaysPharmacologyBinding Sitesbiology010405 organic chemistryChemistryPharmacology. TherapyOrganic ChemistryHydrogen BondingLeishmaniasisbiology.organism_classificationmedicine.diseaseLeishmaniaProtein Structure Tertiary0104 chemical sciencesMolecular Docking Simulation010404 medicinal & biomolecular chemistryChemistryMolecular MedicineBenzimidazolesHuman medicineLeishmania infantumChemical biology and drug design
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