Search results for "41"

showing 10 items of 3365 documents

Density Functional Theory Study of the Trans-Trans-Cis (TTC)→Trans-Trans-Trans (TTT) Isomerization of a Photochromic Spiropyran Merocyanine

2008

Density Functional Theory (DFT) calculations have been performed on the TTC→TTT isomerization reaction of the open forms of the 1',3'-dihydro-8-bromo-6-nitro- 1',3',3'-trimethylspiro[2H-1-benzopyran-2,2'-(2H)indole (8-Br-6-nitro-BIPS) system. The calculations were carried out in vacuo and in methylene chloride solution at different temperatures. Results are compared with the available experimental values of free energy difference and activation energy in solution.

Models MolecularIndolesVacuumSpiropyran; photochromism; DFT calculation; solvent influence on activation energy; merocyanine.merocyaninesolvent influence on activation energyPharmaceutical ScienceDFT calculationPyrimidinonesPhotochemistryArticleAnalytical Chemistrylcsh:QD241-441Photochromismchemistry.chemical_compoundlcsh:Organic chemistryDrug DiscoveryBenzopyransMerocyaninePhysical and Theoretical ChemistryMethyleneFluorescent DyesIndole testSpiropyranMethylene ChlorideOrganic ChemistryStereoisomerismModels TheoreticalNitro CompoundsphotochromismSolutionschemistrymerocyanine.Chemistry (miscellaneous)ThermodynamicsMolecular MedicineDensity functional theorySpiropyranIsomerizationCis–trans isomerismMolecules
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Factors Governing the Chemical Stability and NMR Parameters of Uracil Tautomers and Its 5-Halogen Derivatives

2020

We report on the density functional theory (DFT) modelling of structural, energetic and NMR parameters of uracil and its derivatives (5-halogenouracil (5XU), X = F, Cl, Br and I) in vacuum and in water using the polarizable continuum model (PCM) and the solvent model density (SMD) approach. On the basis of the obtained results, we conclude that the intramolecular electrostatic interactions are the main factors governing the stability of the six tautomeric forms of uracil and 5XU. Two indices of aromaticity, the harmonic oscillator model of aromaticity (HOMA), satisfying the geometric criterion, and the nuclear independent chemical shift (NICS), were applied to evaluate the aromaticity of ur…

Models MolecularMagnetic Resonance SpectroscopyNICSsolvent stabilizationMolecular ConformationPharmaceutical SciencePolarizable continuum modelDFTArticleAnalytical Chemistrylcsh:QD241-441tautomersHalogenslcsh:Organic chemistryComputational chemistryDrug DiscoveryHOMAPhysical and Theoretical ChemistryUracilDensity Functional TheoryBasis setMolecular Structure5-halogenouracil (5XU)ChemistryChemical shiftOrganic ChemistryAromaticityaromaticityTautomerChemistry (miscellaneous)Intramolecular forceSolventsMolecular MedicineChemical stabilityDensity functional theoryMolecules
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(Trifluoromethoxy)Phenylboronic Acids: Structures, Properties, and Antibacterial Activity.

2021

Three isomers of (trifluoromethoxy)phenylboronic acids were studied in the context of their physicochemical, structural, antimicrobial and spectroscopic properties. They were characterized by 1H, 13C, 11B and 19F NMR spectroscopy. The acidity of all the isomers was evaluated by both spectrophotometric and potentiometric titrations. The introduction of the -OCF3 group influences the acidity, depending, however, on the position of a substituent, with the ortho isomer being the least acidic. Molecular and crystal structures of ortho and para isomers were determined by the single crystal XRD method. Hydrogen bonded dimers are the basic structural motives of the investigated molecules in the sol…

Models MolecularMagnetic Resonance SpectroscopyPotentiometric titrationSubstituentMolecular ConformationPharmaceutical ScienceContext (language use)Crystal structureMicrobial Sensitivity TestsDFTMedicinal chemistryArticleOCF<sub>3</sub>Analytical Chemistrylcsh:QD241-441chemistry.chemical_compoundlcsh:Organic chemistryDrug StabilityIsomerismtrifluoromethoxyDrug DiscoveryMoleculePhysical and Theoretical ChemistryMolecular StructureHydrogen bondOrganic ChemistryBoronic AcidsNMRAnti-Bacterial AgentsantibacterialchemistryChemistry (miscellaneous)Intramolecular forceX-RayMolecular MedicineisomersOCF3Derivative (chemistry)Molecules (Basel, Switzerland)
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Synthesis of Pyrrolo[1,2-a]pyrimidine Enantiomers via Domino Ring-Closure followed by Retro Diels-Alder Protocol

2017

From 2-aminonorbornene hydroxamic acids, a simple and efficient method for the preparation of pyrrolo[1,2-a]pyrimidine enantiomers is reported. The synthesis is based on domino ring-closure followed by microwave-induced retro Diels-Alder (RDA) protocols, where the chirality of the desired products is transferred from norbornene derivatives. The stereochemistry of the synthesized compounds was proven by X-ray crystallography. The absolute configuration of the product is determined by the configuration of the starting amino hydroxamic acid. peerReviewed

Models MolecularMagnetic Resonance SpectroscopyPyrimidinehydroxamic acidStereochemistryPharmaceutical ScienceChemistry Techniques SyntheticCrystallography X-RayHydroxamic Acids010402 general chemistryRing (chemistry)01 natural sciencesArticleDominoAnalytical Chemistrymicrowave chemistrylcsh:QD241-441chemistry.chemical_compoundlcsh:Organic chemistryDrug DiscoveryPhysical and Theoretical ChemistryN-heterocyclesta116Norbornenedomino reactions; hydroxamic acid; microwave chemistry; <i>N</i>-heterocycles; retro Diels-Alder reactionHydroxamic acidMolecular Structure010405 organic chemistryretro Diels-Alder reactionOrganic Chemistrydomino reactionsAbsolute configurationStereoisomerism0104 chemical sciencesPyrimidineschemistryChemistry (miscellaneous)Molecular MedicineEnantiomerChirality (chemistry)Molecules; Volume 22; Issue 4; Pages: 613
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Structural, Thermoanalytical and Molecular Modeling Studies on N-(3-hydroxypropyl) 3a,12a-Dihydroxy-5b-cholan-24-amide and Its Monohydrates

2007

The synthetic method for preparing N-(3-hydroxypropyl) 3 alpha,12 alpha-dihydroxy-5 beta-cholan-24-amide can lead to formation of at least three different crystal forms - an anhydrous compound and two monohydrates. The structural and thermal properties of these forms have been characterized by 13C-CP/MAS-NMR and IR spectroscopy, thermo- gravimetry, differential scanning calorimetry and by powder and single crystal x-ray crystallography. In addition, theoretical 13C-NMR chemical shift calculations were also performed for the anhydrous compound and for the first monohydrate, starting from single crystal structures and the structures of these species have now been verified. The first monohydra…

Models MolecularMagnetic Resonance Spectroscopysolid state structure.termoanalyysiPharmaceutical ScienceInfrared spectroscopy13C-CP/MAS-NMR spectroscopy13C-CP/MAS-NMR spektroskopiaFull Research PaperAnalytical ChemistryCrystallcsh:QD241-441Differential scanning calorimetrylcsh:Organic chemistryX-Ray DiffractionDrug Discoverykiinteän tilan rakenneSolid state structurePhysical and Theoretical ChemistrycrystallographyCarbon Isotopeskristallografiathermal Bile acidsCalorimetry Differential ScanningChemistryHydrogen bondOrganic ChemistryTemperatureWaterHydrogen BondingkidetiedeAmidesBile acidsCrystallographysappihapotChemistry (miscellaneous)X-ray crystallographyThermogravimetryAnhydrousCholanesMolecular MedicineOrthorhombic crystal systemSingle crystalthermal analysis
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DesMol2, an Effective Tool for the Construction of Molecular Libraries and Its Application to QSAR Using Molecular Topology

2019

A web application, DesMol2, which offers two main functionalities, is presented: the construction of molecular libraries and the calculation of topological indices. These functionalities are explained through a practical example of research of active molecules to the formylpeptide receptor (FPR), a receptor associated with chronic inflammation in systemic amyloidosis and Alzheimer&rsquo

Models MolecularMultilinear mapQuantitative structure–activity relationshiplinear discriminant analysisComputer scienceQuantitative Structure-Activity RelationshipPharmaceutical ScienceComputational biology01 natural sciencesArticleAnalytical ChemistrySmall Molecule Librarieslcsh:QD241-44103 medical and health scienceslcsh:Organic chemistryDrug DiscoveryPhysical and Theoretical ChemistryPiperazineDesMol2030304 developmental biology0303 health sciencesMolecular Structure010405 organic chemistryOrganic Chemistrymolecular librariesBase (topology)Linear discriminant analysisReceptors Formyl PeptideSystemic amyloidosis0104 chemical sciencestopology descriptorsmultilinear regression analysisDiscriminantChemistry (miscellaneous)Molecular MedicineMultiple linear regression analysisMolecular topologyAlzheimer’s diseaseDatabases ChemicalSoftwareProtein BindingMolecules
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Unveiling the Different Chemical Reactivity of Diphenyl Nitrilimine and Phenyl Nitrile Oxide in [3+2] Cycloaddition Reactions with (R)-Carvone throug…

2020

The [3+2] cycloaddition (32CA) reactions of diphenyl nitrilimine and phenyl nitrile oxide with (R)-carvone have been studied within the Molecular Electron Density Theory (MEDT). Electron localisation function (ELF) analysis of these three-atom-components (TACs) permits its characterisation as carbenoid and zwitterionic TACs, thus having a different reactivity. The analysis of the conceptual Density Functional Theory (DFT) indices accounts for the very low polar character of these 32CA reactions, while analysis of the DFT energies accounts for the opposite chemoselectivity experimentally observed. Topological analysis of the ELF along the single bond formation makes it possible to characteri…

Models MolecularNitrilemolecular mechanismsPharmaceutical Science010402 general chemistrynitrilimines01 natural sciencesArticleAnalytical Chemistrylcsh:QD241-441chemistry.chemical_compoundlcsh:Organic chemistryComputational chemistryDrug DiscoveryNitrilesSingle bondReactivity (chemistry)Physical and Theoretical ChemistryChemoselectivityCarbenoidCycloaddition ReactionMolecular Structure010405 organic chemistryChemistryNitrilimineOrganic ChemistryBiphenyl Compoundsmolecular electron density theory[3+2] cycloadditionsCycloaddition0104 chemical sciencesChemistry (miscellaneous)chemoselectivitynitrile oxidesMolecular MedicineQuantum TheoryDensity functional theoryMolecules
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Mass Spectrometry and Structural Biology Techniques in the Studies on the Coronavirus-Receptor Interaction

2020

Mass spectrometry and some other biophysical methods, have made substantial contributions to the studies on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and human proteins interactions. The most interesting feature of SARS-CoV-2 seems to be the structure of its spike (S) protein and its interaction with the human cell receptor. Mass spectrometry of spike S protein revealed how the glycoforms are distributed across the S protein surface. X-ray crystallography and cryo-electron microscopy made huge impact on the studies on the S protein and ACE2 receptor protein interaction, by elucidating the three-dimensional structures of these proteins and their conformational changes. The…

Models MolecularProtein Conformation alpha-HelicalvirusesGene ExpressionPharmaceutical ScienceReviewPlasma protein bindingSevere Acute Respiratory Syndromemedicine.disease_causeAnalytical Chemistry0302 clinical medicineDrug Discovery030212 general & internal medicineReceptorPeptide sequenceCoronavirus0303 health sciencesChemistrySevere acute respiratory syndrome-related coronavirusBiochemistryChemistry (miscellaneous)Host-Pathogen InteractionsSpike Glycoprotein CoronavirusReceptors VirusMolecular MedicineAngiotensin-Converting Enzyme 2Coronavirus InfectionsProtein BindingglycosylationSARS coronavirusPneumonia Viralstructural techniquesSequence alignmentPeptidyl-Dipeptidase AMass spectrometrylcsh:QD241-441Betacoronavirus03 medical and health scienceslcsh:Organic chemistryspike protein-ACE2 interactionmedicineHumansProtein Interaction Domains and MotifsAmino Acid SequencePhysical and Theoretical ChemistryBinding sitePandemics030304 developmental biologyBinding SitesSARS-CoV-2Organic ChemistryCOVID-19MSStructural biologyProtein Conformation beta-StrandSequence AlignmentMolecules
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Trimeric HIV Env provides epitope occlusion mediated by hypervariable loops

2014

AbstractHypervariable loops of HIV-1 Env protein gp120 are speculated to play roles in the conformational transition of Env to the receptor binding-induced metastable state. Structural analysis of full-length Env-based immunogens, containing the entire V2 loop, displayed tighter association between gp120 subunits, resulting in a smaller trimeric diameter than constructs lacking V2. A prominent basal quaternary location of V2 and V3′ that challenges previous reports would facilitate gp41-independent gp120-gp120 interactions and suggests a quaternary mechanism of epitope occlusion facilitated by hypervariable loops. Deletion of V2 resulted in dramatic exposure of basal, membrane-proximal gp41…

Models MolecularProtein ConformationvirusesHuman immunodeficiency virus (HIV)[CHIM.THER]Chemical Sciences/Medicinal ChemistryPlasma protein bindingHIV Envelope Protein gp120medicine.disease_causeEnv ProteinEpitopeenv Gene ProductsEpitopesProtein structureModelsComputingMilieux_MISCELLANEOUSSequence DeletionGeneticsMultidisciplinary[SDV.BBM.BS]Life Sciences [q-bio]/Biochemistry Molecular Biology/Structural Biology [q-bio.BM]Transition (genetics)biologyenv Gene Products Human Immunodeficiency Virusvirus diseaseshypervariable loopsHIV Envelope Protein gp41[SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry Molecular Biology/Biomolecules [q-bio.BM]3. Good health[SDV.BBM.BS]Life Sciences [q-bio]/Biochemistry Molecular Biology/Biomolecules [q-bio.BM]CD4 AntigensHIV/AIDSAntibodyHuman Immunodeficiency VirusProtein BindingEnvGp41ArticleVaccine RelatedGenetics[CHIM.CRIS]Chemical Sciences/CristallographymedicineHumansProtein Interaction Domains and Motifs[SDV.BBM.BC]Life Sciences [q-bio]/Biochemistry Molecular Biology/Biochemistry [q-bio.BM]AntigensVaccine Related (AIDS)Preventionta1182Molecular[SDV.IMM.IMM]Life Sciences [q-bio]/Immunology/ImmunotherapyCD4Peptide Fragmentsgp120Good Health and Well BeingHIV-1biology.proteinImmunizationProtein MultimerizationproteinScientific Reports
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Unveiling the Lewis Acid Catalyzed Diels–Alder Reactions Through the Molecular Electron Density Theory

2020

The effects of metal-based Lewis acid (LA) catalysts on the reaction rate and regioselectivity in polar Diels&ndash

Models MolecularReaction mechanismDieneChemistry OrganicMolecular ConformationNormal DistributionPharmaceutical ScienceElectrons010402 general chemistry01 natural sciencesArticleAnalytical ChemistryCatalysisReaction ratelcsh:QD241-441chemistry.chemical_compoundNucleophilelcsh:Organic chemistryComputational chemistryDrug DiscoveryButadienesLewis acids and basesPhysical and Theoretical ChemistryLewis Acidsrelation mechanismCycloaddition Reactioncatalysis010405 organic chemistryOrganic Chemistrymolecular electron density theoryRegioselectivityLewis acid0104 chemical sciences3. Good healthchemistryChemistry (miscellaneous)ElectrophileDiels–AlderSolventsMolecular MedicineQuantum TheoryThermodynamicsMolecules
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