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Wyniki wyszukiwania dla: INDOLE-ACRYLONITRILE DERIVATIVES
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Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin
PublikacjaSynthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...
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Ewelina Sokołowska dr hab.
OsobyEwelina Sokołowska, Ph.D. DSc in Economics, Professor of Economics, and Head of the Division of Digital Economy and Finance at the Faculty of Management and Economics at the Gdańsk University of Technology.She holds a master's degree in economics with a specialisation in financial management. She completed her studies at the Faculty of Economic Sciences and Management at the Nicolaus Copernicus University in Toruń, where she defended...
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A convenient and efficient alfa-sulfenylation of carbonyl compounds
PublikacjaA method for alfa-sulfenylation of carbonyl compounds by a 5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinane-2-disulfanyl derivatives has been developed. Readily available reagents, mild reaction conditions, and excellent yields with high selectivity makes this method quite simple, convenient and practical.
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Crank–Nicolson FDTD Method in Media Described by Time-Fractional Constitutive Relations
PublikacjaIn this contribution, we present the Crank-Nicolson finite-difference time-domain (CN-FDTD) method, implemented for simulations of wave propagation in media described by time-fractional (TF) constitutive relations. That is, the considered constitutive relations involve fractional-order (FO) derivatives based on the Grünwald-Letnikov definition, allowing for description of hereditary properties and memory effects of media and processes....
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Convenient and efficient N-methylation of secondary amines under solvent-free ball milling conditions
PublikacjaIn the present work, we report the development of a rapid, efcient, and solvent-free procedure for the N-methylation of secondary amines under mechanochemical conditions. After optimization of the milling parameters, a vibrational ball mill was used to synthesize 26 tertiary N-methylated amine derivatives in a short time of 20 min (30 Hz frequency) and high yields ranging from 78 to 95%. An exception was compounds having a hydroxyl...
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Solving Boundary Value Problems for Second Order Singularly Perturbed Delay Differential Equations by ε-Approximate Fixed-Point Method
PublikacjaIn this paper, the boundary value problem for second order singularly perturbed delay differential equation is reduced to a fixed-point problem v = Av with a properly chosen (generally nonlinear) operator A. The unknown fixed-point v is approximated by cubic spline vh defined by its values vi = vh(ti) at grid points ti, i = 0, 1, ... ,N. The necessary for construction the cubic spline and missing the first derivatives at the boundary...
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Aspects of pollution in Gdansk and gdynia Harbours at the coastal zone of the South Baltic Sea
PublikacjaOrganotin compounds (OTC), as well as metals, are toxic to many organisms. Even at very low concentrations OTC and metals can have several negative effects. The paper discusses key issues relating to the location of harbours in the coastal zone (including near the river mouths and semi-closed access to the sea) and the pollution of harbour sediments with heavy metals (e.g. zinc, copper, nickel and lead) and organotin derivatives...
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Atom-economic thiophosphoroselenenylations of C–H acid esters and amides
PublikacjaThree improved thiophosphoroselenenylation procedures of CHacids, including derivatives of malonic and acetyl-, phosphono-, 4-nitrophenyl- and 3-pyridylacetic acids, have been described and compared to previously reported thiophosphoroselenylation of diethyl malonate using bis(disopropoxyphosphinothioyl)diselenide alone or with the aid of methyl iodide. The use of iodine makes it possible to utilize both equivalents of the selenenylating...
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Thermodynamic Studies of Interactions between Sertraline Hydrochloride and Randomly Methylated β-Cyclodextrin Molecules Supported by Circular Dichroism Spectroscopy and Molecular Docking Results
PublikacjaThe interaction between sertraline hydrochloride (SRT) and randomly methylated β-cyclodextrin (RM β CD) molecules have been investigated at 298.15 K under atmospheric pressure. The method used—Isothermal Titration Calorimetry (ITC) enabled to determine values of the thermodynamic functions like the enthalpy (DH), the entropy (DS) and the Gibbs free energy (DG) of binding for the examined system. Moreover, the stoichiometry coefficient...
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New Analogues of Mycophenolic Acid
PublikacjaMycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: mycophenolate mofetil (MMF,...
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Elżbieta Cecerska-Heryć dr n.med.
OsobyWykształcenie i stopnie naukowe: 19.06.2018 r.ukończenie studiów doktoranckich z wyróżnieniem summa cum laudena Wydziale Lekarskim z OdziałemNauczania w Języku Angielskim PUM SzczecinStopień naukowy: doktor nauk medycznychWyższe2008-2013 Pomorski Uniwersytet Medyczny w Szczecinie Kierunek: Biotechnologia Specjalność: Biotechnologia MedycznaStudia licencjackie i magisterskieZatrudnienie...
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The stereoselective formation of β-lactams with acyl ketenes generated from 5-acyl-Meldrum's acids
PublikacjaAcyl ketenes formed during thermal decompositions of 5-acyl-2,2-dimethyl-1,3-dioxa-4,6-diones undergo stereoselective [2+2] cycloaddition to chiral aldimines. We report the first example of optically active 3-acyl-β-lactams formation from Meldrum’s acid derivatives.
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Applications of Alkanethiols in Organic Synthesis
PublikacjaThis manuscript is an update to the earlier Science of Synthesis contribution describing methods for the synthesis of alkanethiols. Thiols can be converted into sulfonic, sulfinic, sulfenic acid and their derivatives, sulfides, disulfides, polysulfides, sulfonium salts, and thiiranes, etc. These transformations are accomplished by nucleophilic displacement or addition, oxidation, condensation, or coupling reactions involving thiol...
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Synthesis of amides under microwave irradiation
PublikacjaAmides belong to the most important carboxylic acid derivatives. They are constituents of natural compounds like peptides and proteins. They found applications in many branches of science and industry, especially in pharmaceutical and polymer science. Conventional procedures for amide preparation involve reaction between amine and carboxylic acid or their more active derivatives such as acid chlorides, acid anhydrides or esters....
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Copper(II) complexes of 7-amino-2-methylchromone and 7-aminoflavone: Magneto-structural, spectroscopic and DFT characterization
PublikacjaFour new complexes of copper(II) consisting of two different chromone derivatives with carbonyl and amine donor atoms: 7-aminoflavone (L1) and 7-amino-2-methylchromone (L2), were synthesized and characterized by X-ray diffraction, UV–Vis, FT-IR, EPR spectroscopy, MS and elemental analysis. In all four compounds, the chromone derivatives were found to act as monodentate O- or N-ligands. The structural characteristics of 1a and...
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Modulation of CYP1A1, CYP1A2 and CYP1B1 expression by cabbage juices and indoles in human breast cell lines
PublikacjaEpidemiological studies have shown that consumption of cab- bage and sauerkraut is connected with significant reduction of breast cancer incidences. Estrogens are considered a major breast cancer risk factor and their metabolism by P450 enzymes substan- tially contributes to carcinogenic activity. The aim of this study was to investigate the effect of cabbage and sauerkraut juices of differ- ent origin on the expression profile...
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TOTAL CROSS SECTIONS FOR ELECTRON SCATTERING FROM SELECTED HYDROCARBONS: THE SUBSTITUTIONAL AND ADDITIVITY EFFECTS
PublikacjaTotal cross sections (TCS) for electron scattering from selected alkyne molecules, ethylene and its derivatives are compared. All cross sections have been measured in a wide energy range, from about 1 eV up to 370 eV, with the same electrostatic electron spectrometer. The substitutional and additivity effects are indicated and discussed.
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Systems of Nonlinear Fractional Differential Equations
PublikacjaUsing the iterative method, this paper investigates the existence of a unique solution to systems of nonlinear fractional differential equations, which involve the right-handed Riemann-Liouville fractional derivatives D(T)(q)x and D(T)(q)y. Systems of linear fractional differential equations are also discussed. Two examples are added to illustrate the results.
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Unusual behavior of secondary amine group as a leaving group
PublikacjaIn our recent project we focused on reactivity of2,2-dimethyl-4,6-dioxane-1,3-dione carbamoilo- and thiocarbamoylo- derivatives as a ketenesource. Meldrum`s acid derivatives after thermal decomposition gives substituted keteneswith stoichiometric yield, that can be trapped with various spectrum of nucleophiles likealcohols, thiols, amine, imines etc. In case of5-[3-(dimethylamino)-sulfanyl-propyliden]-2,2-dimethyl-1,3-dioxane-4,6-dione...
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Teloxantron inhibits the processivity of telomerase with preferential DNA damage on telomeres
PublikacjaTelomerase reactivation is one of the hallmarks of cancer, which plays an important role in cellular immortalization and the development and progression of the tumor. Chemical telomerase inhibitors have been shown to trigger replicative senescence and apoptotic cell death both in vitro and in vivo. Due to its upregulation in various cancers, telomerase is considered a potential target in cancer therapy. In this study, we identified...
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Calix[4]arenes appended with thioamide moieties as powerful tool for heavy metals recognition
PublikacjaSelectivity of new thioamide derivatives was assessed using those ligands as sensor materials in ion-selective membrane electrodes and tested towards Pb2+ - selectivity. The influence of the nature of the thioamide function (linear, branched or cyclic substituents) on their ionophoric properties was investigated. Electrodes based on cyclic thioamide moieties are promising analytical tools for monitoring Pb2+ concentration in natural...
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Convenient and efficient synthesis of functionalized unsymmetrical alkynyl sulfides
PublikacjaWe developed a simple and efficient method for the synthesis of functionalized unsymmetrical alkynyl sulfides under mild conditions in good yields. The designed method is based on the reaction of 5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-disulfanyl derivatives with lithium acetylides. The developed method allows the preparation of unsymmetrical alkynyl sulfides bearing additional hydroxyl, carboxyl, or amino functionalities.
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Rengel Cane Sia Doctoral Candidate
OsobyI'm Rengel, born and raised in the Philippines. I joined the Gdansk University of Technology in October 2019 as a Maria Skłodowska-Curie early-stage researcher. Calculating the Photophysics of molecular logic sensors for the early detection of atherosclerosis - a precursor to the world's leading causes of death. I'm a professional bass player. I play music to relieve stress and express creativity. I also like reading fantasy...
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The comparison of cytotoxic and genotoxic activities of glucosinolates, isothiocyanates, and indoles
PublikacjaChemopreventive properties of Brassica vegetables are attributed mainly to their characteristic compounds—glucosinolates (GLs) and their main hydrolysis products—isothiocyanates (ITCs) and indoles. In this study, we compared antiproliferative activity (MTT test in HT29 cells) and genotoxic effects (comet assay in HT29 cells and restriction analysis in a cell-free system) of three GLs (sinigrin (SIN), glucotropaeolin (GTL), and...
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Enhanced Toxicity of Bisphenols Together with UV Filters in Water: Identification of Synergy and Antagonism in Three-Component Mixtures
PublikacjaContaminants of emerging concern (CEC) localize in the biome in variable combinations of complex mixtures that are often environmentally persistent, bioaccumulate and biomagnify, prompting a need for extensive monitoring. Many cosmetics include UV filters that are listed as CECs, such as benzophenone derivatives (oxybenzone, OXYB), cinnamates (2-ethylhexyl 4-methoxycinnamate, EMC) and camphor derivatives (4-methylbenzylidene-camphor,...
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Impact of dyes isomerization effect on the charge transfer phenomenon occurring on the dye/nanosemiconductor interface
PublikacjaThe present work aimed to find the answer how does the isomerization of the Ru based dyes affect the overall photon-to-current efficiency of the DSSCs and to explain the charge transfer phenomenon occurring on the dye/ nanosemiconductor interface. Therefore, electronic and optical properties of three bipyridine derivatives anchored on the TiO2 electrode were investigated by computational simulations based on quantum chemistry codes...
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Peptide modification with thiomalonoamide moiety
PublikacjaAbstract: Meldrum acid derivatives under the thermal decomposition are well known source of ketenes. Recently we investigated chemical properties of thiocarbamolyl meldrum acids. We found that 5-(α-alkylamino- α'-sulfhydryl)methylene Meldrum's acids hated in the presence of amines produce thiomalonamides. We used this reaction to the one pot synthesis of series of short peptides containing thiomalonoamide motif.
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Synthesis and Cholinesterase Inhibitory Activity of N-Phosphorylated /N-Tiophosphorylated Tacrine
PublikacjaNovel phosphorus and thiophosphorus tacrine derivatives were designed, synthesized and their biological activity and molecular modeling was investigated as a new potential anti-Alzheimer's disease (AD) agents. All new synthesized compound exhibited lower toxicity against neuroblastoma cell line (SH-SY5Y) in comparison with tacrine. Two analogues in the series, 7 and 9, demonstrated lack of cytotoxicity against hepatocellular cells...
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SYNTHESIS OF PHOSPHORUS TACRINE ANALOGUES AS A NEW POTENTIAL ANTI-ALZHEIMER’S DISEASE AGENTS
PublikacjaA series of novel phosphorus tacrine derivatives was obtained in three steps, including synthesis of 9-chlorotacrine, connection of 9-chlorotacrine with hexamethylenediamine, 1,8-diaminooctane and 1,12-diaminododecane linkers and reaction of obtained tacrine diamine analogues with corresponding acid ester to give nine tacrine organophosphorus compounds. All of the obtained final structures were characterized by 1H NMR, 13C NMR,...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublikacjaFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Encapsulation of an anticancer drug Isatin inside a host nano-vehicle SWCNT: a molecular dynamics simulation
PublikacjaThe use of carbon nanotubes as anticancer drug delivery cargo systems is a promising modality as they are able to perforate cellular membranes and transport the carried therapeutic molecules into the cellular components. Our work describes the encapsulation process of a common anticancer drug, Isatin (1H-indole-2,3-dione) as a guest molecule, in a capped single-walled carbon nanotube (SWCNT) host with chirality of (10,10). The...
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Novel Functionalization of Boron-Doped Diamond by Microwave Pulsed-Plasma Polymerized Allylamine Film
PublikacjaWe report the novel modification of a hydrogen-terminated polycrystalline boron-doped electrode with a microwave pulsed-plasma polymerized allylamine. Boron-doped diamond (BDD) was coated with a very thin layer of adherent cross-linked, pinhole- and additive-free allylamine plasma polymer (PPAAm) resistant to hydrolysis and delamination and characterized by a high density of positively charged amino groups. The pulsed microwave...
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‘Acridines’ as New Horizons in Antifungal Treatment
PublikacjaFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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A convenient method for the preparation of functionalized N-acylsulfenamides from primary amides.
PublikacjaWe have developed a convenient method for the synthesis of functionalized N-acylsulfenamides under mild conditions and in moderate to good yields. The designed method is based on the reaction of (5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinan-2-yl)-disulfanyl derivatives with nitrogen nucleophiles generated from primary amides or imides and sodium hydride. The developed method allows for the preparation of N-acylsulfenamides bearing...
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Non-enzymatic glutathione-mediated conjugation of unsymmetrical bisacridine C-2028 with anticancer activity
Dane BadawczeThe presented data complement the studies on the interplay between C-2028 (anticancer-active unsymmetrical bisacridine) and the glutathione S-transferase/glutathione (GST/GSH) system.
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A Fortran-95 algorithm to solve the three-dimensional Higgs boson equation in the de Sitter space-time
Dane BadawczeA numerically efficient finite-difference technique for the solution of a fractional extension of the Higgs boson equation in the de Sitter space-time is designed. The model under investigation is a multidimensional equation with Riesz fractional derivatives of orders in (0,1)U(1,2], which considers a generalized potential and a time-dependent diffusion...
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Access to Side-On Bonded Tungsten Phosphanylphosphinidene Complexes
PublikacjaMetathesis reactions between diimido complexes of tungsten(VI)[(ArN)2WCl2] (Ar = 2,6-iPr2C6H3) and lithium derivatives of diphosphanes R2P-P(SiMe3)Li (R = tBu and iPr) yield two anionic diimido complexes of tungsten with side-on bonded phosphanylphosphinidene ligands, [(ArN)2WCl(η2-R2P-P)]-. Both complexes are structurally characterized. A possible reaction mechanism and the role of donor solvents are discussed on the basis of...
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Escherichia coli K-12 suppressor-free mutants lacking early glycosyltransferases and late acyltransferases. Minimal lipopolysaccharide structure and induction of envelope stress response.
PublikacjaTo elucidate the minimal lipopolysaccharide (LPS) structure needed for the viability of Escherichia coli, suppressor-free strains lacking either the 3-deoxy-d-manno-oct-2-ulosonic acid transferase waaA gene or derivatives of the heptosyltransferase I waaC deletion with lack of one or all late acyltransferases (lpxL/M/P) and/or various outer membrane biogenesis factors were constructed. Δ(waaC lpxL lpxM lpxP) and waaA mutants exhibited...
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On existence and uniqueness of weak solutions for linear pantographic beam lattices models
PublikacjaIn this paper, we discuss well-posedness of the boundary-value problems arising in some “gradientincomplete” strain-gradient elasticity models, which appear in the study of homogenized models for a large class ofmetamaterials whosemicrostructures can be regarded as beam lattices constrained with internal pivots. We use the attribute “gradient-incomplete” strain-gradient elasticity for a model in which the considered strain energy...
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Advanced oxidation processes for the removal of mono and polycyclic aromatic hydrocarbons – A review
PublikacjaAromatic hydrocarbons (AHs) are toxic environmental contaminants presented in most of the environmental matrices. Advanced oxidation processes (AOPs) for the removal of AHs in the account of complete mineralization from various environmental matrices have been reviewed in this paper. An in-depth discussion on various AOPs for mono (BTEX) and polyaromatic hydrocarbons (PAHs) and their derivatives is presented. Most of the AOPs were...
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Chalcogen bonding interactions in a series of aromatic selenocyanates
PublikacjaSelenium atoms in aromatic selenocyanates are characterized by the occurrence of two σ-holes, a stronger one in the prolongation of the NC–Se bond and a weaker one in the prolongation of the Ar–Se bond. The crystal structures of several bis(selenocyanato) derivatives, prepared by a method originally developed for ortho bis-substituted derivatives, illustrate very well this difference, with a short NC–Se⋯NC ChB interaction organizing...
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublikacjaThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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Molecular dynamics simulations of the affinity of chitin and chitosan for collagen: the effect of pH and the presence of sodium and calcium cations
PublikacjaChitosan and chitin are promising biopolymers used in many areas including biomedical applications, such as tissue engineering and viscosupplementation. Chitosan shares similar properties with hyaluronan, a natural component of synovial fluid, making it a good candidate for joint disease treatment. The structural and energetic consequences of intermolecular interactions are crucial for understanding the biolubrication phenomenon...
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CHARACTERISATION OF CHITOSAN/HYALURONIC ACID BLEND FILMS MODIFIED BY COLLAGEN
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INFLUENCE OF THE INTERMOLECULAR INTERACTION ON PHYSICO-CHEMICAL PROPERTIES OF CHITOSAN/HYALURONIC ACID BLENDS
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THE INFLUENCE OF THE TYPE SOLVENT ON THE STRUCTURE OF CHITOSAN BLENDS WITH HYALURONIC ACID
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EFFECT OF CHITOSAN AND LIPID LAYERS DEPOSITED ONTO POLYETHYLENE TEREPHTHALATE (PET) ON ITS WETTING PROPERTIES
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WETTABILITY OF HYBRID CHITOSAN/PHOSPHOLIPID COATINGS
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WETTABILITY OF CHITOSAN-MODIFIED AND LIPID/POLYPEPTIDE-COATED PEEK SURFACES
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SURFACE CHARACTERISTICS OF DPPC MONOLAYERS DEPOSITED FROM TITANIUM DIOXIDE–CHITOSAN–HYALURONIC ACID SUBPHASES ON A GLASS SUPPORT
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