Search results for "Derivative"

showing 10 items of 1074 documents

Prediction of Aquatic Toxicity of Benzene Derivatives to Tetrahymena pyriformis According to OECD Principles

2016

Background: Many QSAR studies have been developed to predict acute toxicity over several biomarkers like Pimephales promelas, Daphnia magna and Tetrahymena pyriformis. Regardless of the progress made in this field there are still some gaps to be resolved such as the prediction of aquatic toxicity over the protozoan T. pyriformis still lack a QSAR study focused in accomplish the OECD principles. Methods: Atom-based quadratic indices are used to obtain quantitative structure-activity relationship (QSAR) models for the prediction of aquatic toxicity. Our models agree with the principles required by the OECD for QSAR models to regulatory purposes. The database employed consists of 392 substitut…

PharmacologyQuantitative structure–activity relationshipTetrahymena pyriformisAntiprotozoal AgentsQuantitative Structure-Activity Relationship010501 environmental sciencesBiology01 natural sciencesAcute toxicity0104 chemical sciencesAquatic toxicologyToxicology010404 medicinal & biomolecular chemistryParasitic Sensitivity TestsTest setDrug DiscoveryBenzene derivativesLinear regressionTetrahymena pyriformisBenzene DerivativesBiological systemMonte Carlo MethodAlgorithmsBootstrapping (statistics)0105 earth and related environmental sciencesCurrent Pharmaceutical Design
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The conformational properties of dehydrobutyrine and dehydrovaline: theoretical and solid-state conformational studies

2010

Dehydrobutyrine is the most naturally occurring dehydroamino acid. It is also the simplest dehydroamino acid having the geometrical isomers E/Z. To investigate its conformational properties, a theoretical analysis was performed on N-acetyl-α,β-dehydrobutyrine N′-methylamides, Ac-(E)-ΔAbu-NHMe and Ac-(Z)-ΔAbu-NHMe, as well as the dehydrovaline derivative Ac-ΔVal-NHMe. The ϕ, ψ potential energy surfaces and the localised conformers were calculated at the B3LYP/6-311 + + G(d,p) level of theory both in vacuo and with inclusion of the solvent (chloroform, water) effect (SCRF method). The X-ray crystal structures of Ac-(Z)-ΔAbu-NHMe and Ac-ΔVal-NHMe were determined at 85 and 100 K, respectively. …

Pharmacologychemistry.chemical_classificationAlanineDouble bondStereochemistryOrganic ChemistryPeptideGeneral MedicineCrystal structureBiochemistrychemistry.chemical_compoundCrystallographychemistryStructural BiologyDrug DiscoverySide chainMolecular MedicineMolecular BiologyConformational isomerismCis–trans isomerismDerivative (chemistry)Journal of Peptide Science
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Neoclerodane Diterpenoids from Scutellaria pontica

1997

Seven novel neoclerodane diterpenoids, scupontins A-G, have been isolated from the Me2CO extract of the aerial parts of Scutellaria pontica (1-7), together with the known neoclerodanes scutalbin A and scutalpin M. Structures 1-7 were established by exhaustive NMR spectroscopic studies and chemical transformations. Scupontins A-D(1-4, respectively) and scupontins E (5)andF(6) possess unusual [(3¢S,3¢¢S)-3¢-[(3¢¢-acetoxybutyryl)oxy]butyryloxy and [(3¢S,3¢¢S,3¢¢¢S)- 3¢-[[3¢¢-[(3¢¢¢-hydroxybutyryl)oxy]butyryl]oxy]butyryl]oxy substituents, respectively, attached to the C-19 position of the neoclerodane framework. In the case of the 6R,7â-dibenzoate derivative 7 (scupontin G) its absolute config…

Pharmacologychemistry.chemical_classificationBicyclic moleculebiologyStereochemistryOrganic ChemistryAbsolute configurationPharmaceutical ScienceEpoxidebiology.organism_classificationAnalytical Chemistrychemistry.chemical_compoundComplementary and alternative medicinechemistryDrug DiscoveryScutellariaMolecular MedicineDiterpeneChirality (chemistry)Derivative (chemistry)LactoneJournal of Natural Products
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Preparation of 7-Alkoxylated Furanopyrones:  Semisynthesis of (−)-Etharvensin, a New Styryl-Lactone from Goniothalamus arvensis

1997

A new furanopyrone derivative, (−)-etharvensin (1), was isolated from the stem bark of Goniothalamus arvensis. Semisynthesis of the 7-ethoxyfuranopyrone 1 was achieved by addition of EtOH in concentrated acid medium to the unsaturated α-pyrone (+)-altholactone (2). This protocol constitutes a novel, direct (single-step), and efficient method to prepare this class of bioactive compounds.

Pharmacologychemistry.chemical_classificationStem barkbiologyStereochemistryOrganic ChemistryPharmaceutical Sciencebiology.organism_classificationSemisynthesisAnalytical Chemistrychemistry.chemical_compoundComplementary and alternative medicinechemistryDrug DiscoveryMolecular MedicineDerivative (chemistry)EtharvensinGoniothalamusLactoneJournal of Natural Products
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10-Oximeguanacone, the First Nitrogenated Acetogenin Derivative Found To Be a Potent Inhibitor of Mitochondrial Complex I

1998

A new 10-keto bis-tetrahydrofuran acetogenin, guanacone (1), has been isolated from a cytotoxic extract of Annona aff. spraguei seeds. The 10-oximeguanacone derivative 1f is the first bioactive nitrogenated acetogenin found to be a very potent inhibitor of complex I. In addition, a SAR study of guanacone analogues is reported based on the titration of the NADH oxidase and NADH:ubiquinone oxidoreductase activities.

Pharmacologychemistry.chemical_classificationStereochemistryOrganic ChemistryPharmaceutical ScienceBiological activityBiologyAnalytical Chemistrychemistry.chemical_compoundEnzymeComplementary and alternative medicinechemistryEnzyme inhibitorOxidoreductaseDrug DiscoveryAcetogeninbiology.proteinMolecular MedicineLactoneDerivative (chemistry)Heart metabolismJournal of Natural Products
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Triterpene Saponins from Wisteria floribunda “macrobotrys” and “rosea”

2017

Five oleanane-type saponins were isolated from two cultivars of Wisteria floribunda (Willd.) DC. (Fabaceae): From the roots of Wisteria floribunda “macrobotrys”, one new oleanane derivative elucidated as 3- O-β-D-xylopyranosyl-(1→2)-β-D-glucuronopyranosyl-22- O-acetyl-3p,22p,24-trihydroxyolean-12-en-30-oic acid, and two known glycosides, and from the roots of Wisteria floribunda “rosea”, two known ones. Their structures were elucidated by a detailed 600 MHz NMR analysis including 1D and 2D NMR (1H, 13C, COSY, TOCSY, ROESY, HSQC, HMBC) experiments and mass spectrometry. Chemotaxonomic conclusions were proposed.

Pharmacologychemistry.chemical_classificationTraditional medicinebiology010405 organic chemistryPlant ScienceGeneral MedicineFabaceaeWisteria floribundabiology.organism_classification01 natural sciences0104 chemical sciences010404 medicinal & biomolecular chemistrychemistry.chemical_compoundPlant scienceComplementary and alternative medicinechemistryTriterpeneDrug DiscoveryOleananeDerivative (chemistry)Natural Product Communications
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A 18F-labeled dibenzocyclooctyne (DBCO) derivative for copper-free click labeling of biomolecules

2016

The new prosthetic group 18F-TEG-DBCO (dibenzocyclooctyne) can be prepared within a total reaction time of 60 min including purification with an overall yield (n.d.c.) of 34 ± 5%. Copper-free click cycloadditions with an azido-cRGD, a folate-azide and two α-MSH analogue azido-peptides resulted in very high RCYs and fast reaction kinetics.

Pharmacologychemistry.chemical_classificationbiology010405 organic chemistryBiomoleculeOrganic ChemistryPharmaceutical Sciencechemistry.chemical_element010402 general chemistry01 natural sciencesBiochemistryCombinatorial chemistryCopperCofactor0104 chemical sciencesChemical kineticschemistry.chemical_compoundchemistryYield (chemistry)Drug Discoverybiology.proteinMolecular MedicineDerivative (chemistry)MedChemComm
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The Reactivity of 4’-Substituted Spiro[Isoindole-1,3’-pyrazoles] Derivatives: Substitution/Elimination Reactions and Access to Biaryl Derivatives

2017

This paper describes aspects of the chemistry of 4’-substituted spiro [indole-1,3’-pyrazoles]. These compounds underwent substitution and/or elimination reactions to afford some new spiro- as well as biaryl derivatives of potential pharmaceutical relevance. Mechanistic considerations are discussed as well.

Pharmacologychemistry.chemical_compoundElimination reaction4’-substituted spiro [indole-13’-pyrazoles] elimination reactions biaryl derivatives Mechanistic considerationschemistryOrganic ChemistrySubstitution (logic)Reactivity (chemistry)Settore CHIM/06 - Chimica OrganicaIsoindoleSettore CHIM/08 - Chimica FarmaceuticaCombinatorial chemistryAnalytical ChemistryHETEROCYCLES
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Connecting Berry's phase and the pumped charge in a Cooper pair pump

2003

The properties of the tunnelling-charging Hamiltonian of a Cooper pair pump are well understood in the regime of weak and intermediate Josephson coupling, i.e. when $E_{\mathrm{J}}\lesssim E_{\mathrm{C}}$. It is also known that Berry's phase is related to the pumped charge induced by the adiabatical variation of the eigenstates. We show explicitly that pumped charge in Cooper pair pump can be understood as a partial derivative of Berry's phase with respect to the phase difference $\phi$ across the array. The phase fluctuations always present in real experiments can also be taken into account, although only approximately. Thus the measurement of the pumped current gives reliable, yet indirec…

Phase differencePhysicsSuperconductivityCondensed Matter - SuperconductivityFOS: Physical sciencesObservableSuperconductivity (cond-mat.supr-con)symbols.namesakeQuantum mechanicssymbolsPartial derivativeCooper pairHamiltonian (quantum mechanics)Eigenvalues and eigenvectors
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In-Plane Anisotropy and Phase Change in Langmuir-Blodgett Films of a Triphenylene Derivative

1993

Abstract The “in-plane anisotropy” of a triphenylene derivative in Langmuir-Blodgett (L.B.) films has been investigated. Upon heating, L.B. films exhibit a reversible phase transition appearing as an abrupt increase from a low to a high “in-plane anisotropy” corresponding to the formation of the same hexagonal liquid crystal phase observed in the bulk material at almost the same temperature, with the columnar axis aligned along the dipping direction.

Phase transitionCondensed matter physicsChemistryTriphenyleneCondensed Matter PhysicsPhotochemistryLangmuir–Blodgett filmCondensed Matter::Soft Condensed Matterchemistry.chemical_compoundIn planeLiquid crystalCondensed Matter::SuperconductivityPhase (matter)AnisotropyDerivative (chemistry)Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals
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