Search results for "Aminoacid"

showing 10 items of 39 documents

N-valproyl-L-tryptophan for CNS-targeting: synthesis, characterization and efficacy in vitro studies of a new potential antiepileptic drug.

2010

A new aminoacidic derivative of valproic acid (VPA) has been synthesized and characterized by analytical and spectral data. The rationale for the preparation of such potential antiepileptic agent is based on the observation that chemical combination of the anticonvulsant pharmacophore, VPA with essential aminoacids could afford more effective and less toxic actives. The synthesis, characterization, physico-chemical parameters functional for crossing Blood Brain Barrier of N-valproyl-L-tryptophan (4) are reported. The Log D pH7.4 (0.3) indicates that (4) is adequate to cross biological membranes. Its chemical and enzymatic stability were assessed. The experiments indicate high stability of c…

Malemedicine.medical_treatmentHippocampal formationPharmacologyIn Vitro TechniquesBlood–brain barrierSettore BIO/09 - FisiologiaHippocampuschemistry.chemical_compoundDrug StabilityIn vivoDrug DiscoverymedicineAnimalsRats WistarValproic AcidEpilepsyDipeptidesAminoacidic derivative Antiepileptic Drug CNS-Targeting Enzymatic Stability Seizure Like Events Model Valproic acidIn vitroElectrophysiological PhenomenaRatsmedicine.anatomical_structureAnticonvulsantchemistrySettore CHIM/09 - Farmaceutico Tecnologico ApplicativoAnticonvulsantsPharmacophoreDerivative (chemistry)medicine.drugMedicinal chemistry (Shariqah (United Arab Emirates))
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Low-Q peak in X-ray patterns of choline-phenylalanine and homophenylalanine: a combined effect of chain and stacking

2016

Abstract In this contribution we report for the first time the X-ray patterns of choline-phenylalanine and choline-homophenylalanine ionic liquids. The presence of a low Q peak in both systems is another evidence that a long alkyl chain is not always needed to establish a nanodomain segregation in the liquid sufficient to be revealed by the diffraction experiment. These new data are compared with the diffraction patterns and the theoretical calculations of other choline-aminoacid ionic liquids recently reported. A significant role might be played by the stacking interactions between aromatic rings.

DiffractionChemical substancePhenylalanineStackingGeneral Physics and AstronomyPhenylalanine02 engineering and technologyIonic liquid010402 general chemistry01 natural sciencesCholinePhysics and Astronomy (all)chemistry.chemical_compoundAminoacidSettore CHIM/02Organic chemistryPhysical and Theoretical ChemistryAlkylcholine-amino acid ionic liquids EDXD; ion pairs; pre-peak; renewable materialschemistry.chemical_classificationSmall-angle X-ray scatteringSAXS; Choline; Phenylalanine; Aminoacids; Ionic liquidsAromaticitySAXS021001 nanoscience & nanotechnologyIonic liquids0104 chemical sciencesCrystallographychemistryIonic liquid0210 nano-technologyAminoacids
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Complexes of diorganotin(IV) with aminoacids and a dipeptide. Synthesis and structural investigations.

2008

The aim of this work is to synthesize complexes of Arginine, effector of recognition, with organotin(IV) ions (R2Sn2+, R =Me, nBu) which are known to possess antitumour, antimicrobial, anti-inflammatory activities. The complexes were investigated by FT-IR and 119Sn Můssbauer.While identical stoichiometries are present for Me2Sn(Arg)2 and Me2Sn(Boc-Arg)2 complexes, 119Sn Můssbauer spectra give a clear evidence of different coordination modes. L-Arginine appears to behave as a chelating ligand through carboxylate and a-NH2 groups in the former, while in Nα-Boc-L-Arginine complex, the Nα-protected amino group being exempted from coordination, only the carboxylate groups are effectors of bondin…

Diorganotin (IV) complexes aminoacids and dipeptideSettore CHIM/03 - Chimica Generale E Inorganica
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HYBRID SYSTEMS FOR TISSUE ENGINEERING

2009

Settore CHIM/09 - Farmaceutico Tecnologico Applicativocomposite scaffolds tissue engineering hyaluronic acid polyaminoacids
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Composite nanoparticles based on hyaluronic acid chemically cross-linked with alpha,beta-polyaspartylhydrazide.

2007

In this paper, new composite nanoparticles based on hyaluronic acid (HA) chemically cross-linked with alpha,beta polyaspartylhydrazide (PAHy) were prepared by the use of a reversed-phase microemulsion technique. HA-PAHy nanoparticles were characterized by FT-IR spectroscopy, confirming the occurrence of the chemical cross-linking, dimensional analysis, and transmission electron micrography, showing a sub-micrometer size and spherical shape. Zeta potential measurements demonstrated the presence of HA on the nanoparticle surface. A remarkable affinity of the obtained nanoparticles toward aqueous media that simulate some biological fluids was found. Stability studies showed the absence of chem…

Polymers and PlasticsBiocompatibilityCell SurvivalNanoparticleBioengineeringAntineoplastic AgentsPolymeric nanoparticles hyaluronic acid polyaminoacidBiomaterialschemistry.chemical_compoundDrug Delivery SystemsMicroscopy Electron TransmissionPolymer chemistryHyaluronic acidSpectroscopy Fourier Transform InfraredMaterials ChemistryZeta potentialHumansMicroemulsionHyaluronic AcidParticle SizeChemical decompositionChemistryHydrolysisEquipment DesignNylonsCross-Linking ReagentsHydrazinesChemical engineeringNanoparticlesFluorouracilDrug carrierK562 CellsNanogelBiomacromolecules
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NANOTECHNOLOGIES FOR BIOMEDICAL APLICATIONS

2010

DRUG DELIVERY SYSTEMS POLYAMINOACIDS NANOMEDICINESettore CHIM/09 - Farmaceutico Tecnologico Applicativo
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Streoselective hemisynthesis of heterosubstituted aminoacidsApplication on radiofluorolabeling for peptide imaging.

2017

Stereoselective hemisynthesis of lateral chain heterosubstituted aminoacids.Applications on radiofluorolabeling for peptide imaging.This thesis work, which was carried out at the Institute of Molecular Chemistry of the University of Burgundy and in collaboration with the Institute of Cognitive and Integrative Neurosciences of Aquitaine, focuses on the development of new methods for the synthesis of side chain heterosubstituted amino acids including phosphine containing or silyl groups, as well as on their applications. In a first part, the synthesis of side chain silylated amino acids is achieved without racemization using a key Wittig reaction between a phosphonium salt, derived from L-asp…

[CHIM.ORGA]Chemical Sciences/Organic chemistryPhosphoniumsSilanesTriazoles[CHIM.ORGA] Chemical Sciences/Organic chemistry[18F]-RadiofluorationPhosphoniumAminoacidsAcides aminés
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Partially competitive inhibition of intestinal baclofen absorption by beta-alanine, a nonessential dietary aminoacid.

1991

In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption rate pseudoconstants of the spasmolytic drug decrease as beta-alanine concentration increases, until a limiting value is obtained (36.8 per cent of that found for baclofen alone). A computer method was developed in order to calculate parameters governing baclofen absorption in the presence of beta-aminoacid, with the following results: Vm = 11.22 mM h-1; Km = 7.42 mM; Ki = 2.4…

Absorption (pharmacology)MaleBaclofenStereochemistryPharmaceutical Sciencebeta-AlanineMichaelis–Menten kineticsIntestinal absorptionchemistry.chemical_compoundNon-competitive inhibitionPharmacokineticsIntestine SmallAnimalsPharmacology (medical)Drug InteractionsPharmacologyChromatographyWaterRats Inbred StrainsGeneral MedicineRatsDietary aminoacidBaclofenchemistryIntestinal Absorptionbeta-AlanineBiopharmaceuticsdrug disposition
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Spaghetti Enriched with Inulin: Effect of Polymerization Degree on Quality Traits and α-Amylase Inhibition.

2022

Inulin is considered a dietary fiber and represents a noteworthy ingredient for food biofortification due to its health effects and its neutral taste. The aim of the work was the evaluation of the quality of pasta produced using whole-meal flours of two ancient Sicilian landraces (Senatore Cappelli-CAP and Timilia—TIM) fortified with two types of inulin (long-chain topinambur inulin IT and low-chain chicory inulin IC), at two different levels of substitution (2 and 4%) to evaluate its possible effect on α-amylase inhibition. The color indices L* and a* were mainly influenced by cultivars, while IT improved the sensory attributes, mainly the elasticity sensation, and influenced l…

inulin; durum wheat; Sicilian landraces; spaghetti; quality; aminoacids; glycemic index; α amylase? amylaseSettore CHIM/10 - Chimica Degli AlimentiSicilian landracesOrganic ChemistryFlourInulinPharmaceutical Sciencedurum wheataminoacidsAnalytical ChemistryPolymerizationα amylaseChemistry (miscellaneous)qualityDrug DiscoveryMolecular Medicineglycemic indexCookingPhysical and Theoretical ChemistrySicilian landracealpha-AmylasesaminoacidspaghettiTriticumMolecules (Basel, Switzerland)
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Unexplored nucleophilic ring opening of aziridines.

2010

The reactivity of dianions of carboxylic acids towards aziridines has been studied. Although, a similar reactivity to that of enolates from ketones, esters or amides has been observed, the method directly yields g-aminoacids in one step. The method is complementary of previous results of enenediolate reactivity with other electrophiles. A comparative study with the reactivity of this enediolates with epoxides is included.

enediolatePharmaceutical ScienceRing (chemistry)ArticleAnalytical Chemistrylcsh:QD241-441lcsh:Organic chemistryNucleophileDrug DiscoveryOrganic chemistryReactivity (chemistry)Physical and Theoretical ChemistryAmino AcidsChemistryOrganic Chemistryγ-aminoacidsRegioselectivityg-aminoacidsKetonesdiastereoselectivityChemistry (miscellaneous)aziridinesregioselectivityElectrophileMolecular MedicineEpoxy CompoundsMolecules (Basel, Switzerland)
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