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Wyniki wyszukiwania dla: chiral pharmaceuticals
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Influence of salinity on the consistency and swelling characteristics of bentonite
PublikacjaRaport z badań eksperymentalnych odnośnie konsystencji bentonitu (wskaźniki plastyczności, stopień plastyczności) i zjawiska pęcznienia (ciśnienie pęcznienia) przedstawiono w zależności od różnych poziomów zasolenia wody.
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublikacjaThe series of 16 novel amino acid and peptide mycophenolic acid (MPA) derivatives was obtained as potential antibacterial agents. Coupling of MPA with respective amines was optimized with condensing reagents such as EDCI/DMAP and T3P/TEA. Amino acid analogs were received both as methyl esters and also with the free carboxylic group. The biological activity of the products was tested on five references bacterial strains: Klebsiella...
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Thermally activated persulfate-based Advanced Oxidation Processes — recent progress and challenges in mineralization of persistent organic chemicals: a review
PublikacjaThermally activated persulfate (TAP) finds application in Advanced Oxidation Processes for the removal of pollutants from contaminated water and soil. This paper reviewed the various cases of TAP in the environmental remediation. The pollutants such as individual pharmaceuticals, biocides, cyclic organic compounds, and dyes are considered in this review. It is interesting to note that most of the organic compounds undergo complete...
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Metody syntezy 2,2'-bipirolidyny
PublikacjaDiaminy wicynalne należą do obszernej grupy związków posiadających dwie grupy aminowe przyłączone do sąsiednich atomów węgla. Są to substancje bardzo zróżnicowane pod względem budowy jak i właściwości chemicznych. Ugrupowanie 1,2-diaminowe obecne jest w wielu związkach wykazujących aktywność biologiczną. W syntezie organicznej 1,2- diaminy, głównie pochodne 1,2-diaminocykloheksanu, stanowią substraty w reakcjach prowadzących do...
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Alternative method for the synthesis of imidazo[5,1-f][1,2,4]triazin-4(3H)-one—a substrate for the preparation of phosphodiesterase (5) inhibitors
PublikacjaImidazo[5,1-f][1,2,4]triazin-4(3H)-ones, as isosteres of purine, are of interest for pharmaceutical research as potential substrates for the synthesis of cGMP-PDE5 inhibitors. We present a novel, alternative method for the synthesis of imidazotriazinones, that differs from the previously reported ones with respect to the method of construction of the triazinone ring in the molecule. The key step in our approach is condensation...
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FTIR, Raman spectroscopy and HT-XRD in compatibility study between naproxen and excipients
PublikacjaDetection of incompatibility between an active pharmaceutical ingredient (API) and excipients, including the selection of the most biopharmaceutical advantageous excipients is extremely important in the pre-formulation process of developing a solid dosage form technology. Therefore, having fast and reliable methods for identifying incompatibility is fundamental in pharmaceutical technology. For this purpose, combined Fourier transform...
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Human serum interactions with phenolic and aroma substances of Kaffir(Citrus hystrix) and Key lime (Citrus aurantifolia) juices
PublikacjaTo understand the therapeutic application of polyphenols extracted from Kaffir (PolKaf) and Key (PolKey) limesdifferent analytical methods were applied. Based on quantitative analysis by two dimensional gas chromato-graphy (GC×GC) and time of flight mass spectrometry (TOFMS) it can be observed that the biggest differencesin the contents of selected terpenes of Kaffir and Key limes occur in chemical compounds such as limonene, citraland...
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The possibility of use keratin products in various branches of industry
PublikacjaBird's feather, the main by-product of the poultry industry, are not enough utilized and negatively influencing the environment. They contain large amount of keratin, the protein with high cystine content. The aim of our work was to obtain hydrolysates and isolates of keratin, which can be used in various areas of food, cosmetics, pharmaceutical industry and as animal feed. Keratin can be hydrolyzed and extracted from feather after...
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Radar Signal Parameters Estimation Using Phase Accelerogram in the Time-Frequency Domain
PublikacjaRadar signal parameter estimation, in the context of the reconstruction of the received signal in a passive radar utilizing other radars as a source of illumination, is one of the fundamental steps in the signal processing chain in such a device. The task is also a crucial one in electronic reconnaissance systems, e.g. ELINT (Electronic Intelligence) systems. In order to obtain accurate results it is important to measure, estimate...
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The optimisation of analytical parameters for routine profiling of antioxidants in complex mixture by HPLC coupled post-column derivatisation
PublikacjaIntroduction: The wide application of natural and artificial antioxidants in food, cosmetic and pharmaceutical industry as well as the recognition of the importance of food antioxidants for supporting human health created demand for reliable and industrially applicable methods of determining antioxidative activity. This requirement can be fullfilled with the recently proposed HPLC-post-column derivatisation approach enabling the...
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Long-Term Stability of Benzodiazepines and Z-Hypnotic Drugs in Blood Samples Stored at Varying Temperatures
PublikacjaBenzodiazepines (BZDs) and Z-drugs are among the most commonly prescribed pharmaceuticals in the world and are considered standard care for various mental illnesses and for treatment of sleeping and anxiety disorders, alcohol withdrawal, muscle spasms and epilepsy. Some BZDs are not allowed as pharmaceuticals in many countries, and they are used as "designer benzodiazepines" (DBZDs). All these compounds are typically screened in...
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Liniowe i nieliniowe modele wielowymiarowej kalibracji do predykcji stężenia substancji z pomiarów woltamperometrycznych
PublikacjaPomiary woltamperometryczne znajdują zastosowanie w wielu dziedzinach nauki i techniki, np. w przemyśle farmaceutycznym. Dane uzyskane w wyniku takich pomiarów zawierają informację odnośnie rodzaju i stężenia badanej substancji, jednakże są one często kłopotliwe w bezpośredniej interpretacji. Z tego powodu, istnieje konieczność wykorzystania odpowiednich metod matematycznych, które umożliwiają uzyskanie bezpośredniej i precyzyjnej...
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Predicting sulfanilamide solubility in the binary mixtures using a reference solvent approach
PublikacjaBackground. Solubility is a fundamental physicochemical property of active pharmaceutical ingredients. The optimization of a dissolution medium aims not only to increase solubility and other aspects are to be included such as environmental impact, toxicity degree, availability, and costs. Obtaining comprehensive...
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Antioxidants: a premature scientific hypothesis that reshuffled the traditional food pyramid
PublikacjaAntioxidants present in substantial amounts in foods, plant-based products in particular, have been suggested as chemopreventive agents that can curb the development of undesirable health effects caused by oxidative stress simply by enriching diet in such compounds. This idea has been enthusiastically accepted by consumers, as well as food and pharmaceutical industry, and created great demand for products containing antioxidant...
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Volute scroll as an alternative to guide vanes at inlet to turbine.
PublikacjaW pracy przedstawiono alternatywny sposób zasilania turbin parowych poprzez zastosowanie podwójnej spirali zasilającej. Przedstawiono model jednowymiarowy obliczania przepływu przez spirale oraz zamieszczono wyniki obliczeń typu 3D. Pokazano jak zależy parametr nierównomierności rozkładu prędkości na wylocie od sposobu kształtowania przekroju spiral.
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Development and Validation of a Gas Chromatography Method for the Trace Level Determination of Allylamine in Sevelamer Hydrochloride and Sevelamer Carbonate Drug Substances
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Structural Characterization and in Vivo Evaluation of β-Hairpin Peptidomimetics as Specific CXCR4 Imaging Agents
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Reversed-Phase TLC and HPLC Retention Data in Correlation Studies with in Silico Molecular Descriptors and Druglikeness Properties of Newly Synthesized Anticonvulsant Succinimide Derivatives
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99mTc-Galacto-RGD2: A Novel 99mTc-Labeled Cyclic RGD Peptide Dimer Useful for Tumor Imaging
PublikacjaThis study sought to evaluate [99mTc(HYNIC-Galacto-RGD2)-(tricine)(TPPTS)] (99mTc-Galacto-RGD2: HYNIC = 6-hydrazinonicotinyl; Galacto-RGD2 = Glu[cyclo[Arg-Gly-Asp-D-Phe-Lys(SAA-PEG2-(1,2,3-triazole)-1-yl-4-ethylamide)]]2 (SAA = 7-amino-L-glycero-L-galacto-2,6-anhydro-7-eoxyheptanamide, and PEG2 = 3,6-dioxaoctanoic acid); and TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) as a new radiotracer for tumor imaging. Galacto-RGD2...
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Microemulsion Delivery Systems with Low Surfactant Concentrations: Optimization of Structure and Properties by Glycol Cosurfactants
PublikacjaExtensive use of microemulsions as delivery systems raises interest in the safe ingredients that can form such systems. Here, we assessed the use of two glycols, i.e., propylene glycol and pentylene glycol, and their mixtures to manipulate the properties and structure of microemulsions. Obtained systems with glycols were extensively characterized in terms of capacity to incorporate water phase, droplet size, polydispersity, structure...
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Encapsulation of Amikacin into Microparticles Based on Low-Molecular-Weight Poly(lactic acid) and Poly(lactic acid-co-polyethylene glycol)
PublikacjaThe aim of this study was to fabricate novel microparticles (MPs) for efficient and long-term delivery of amikacin (AMI). The emulsification method proposed for encapsulating AMI employed low-molecular-weight poly(lactic acid) (PLA) and poly(lactic acid-co-polyethylene glycol) (PLA−PEG), both supplemented with poly(vinyl alcohol) (PVA). The diameters of the particles obtained were determined as less than 30 μm. Based on an in-vitro...
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Mechanism of Binding of Antifungal Antibiotic Amphotericin B to Lipid Membranes: An Insight from Combined Single-Membrane Imaging, Microspectroscopy, and Molecular Dynamics
PublikacjaAmphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design safer derivatives. As the drug primarily targets the biomembranes of both fungi and humans, new insights into the...
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Physical and Mechanical Evaluation of Silicone-Based Double-Layer Adhesive Patch Intended for Keloids and Scar Treatment Therapy
PublikacjaGrowing interest in silicone elastomers for pharmaceutical purposes is due to both theirbeneficial material effect for scar treatment and their potential as drug carriers. Regarding their morphological structure, silicone polymers possess unique properties, which enable a wide range of applicability possibilities. The present study focused on developing a double-layer adhesive silicone film (DLASil) by evaluating its physical...
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Application of vibrational spectroscopy, thermal analyses and X-Ray diffraction in the rapid evaluation of the stability in solid-state of ranitidine, famotidine and cimetidine
PublikacjaThis paper reports the study on applicability of Fourier transform infrared (FTIR), near-infrared (NIR) and Raman spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) for the estimation of the chemical stability and photostability of histamine H2-receptor antagonist substances. Ranitidine hydrochloride (RAN), famotidine (FAM) and cimetidine (CIM) were tested and differences in sensitivity were measured...
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Phytoremediation—From Environment Cleaning to Energy Generation—Current Status and Future Perspectives
Publikacja:Phytoremediationis a technology based on the use of green plants to remove, relocate, deactivate, or destroy harmful environmental pollutants such as heavy metals, radionuclides, hydrocarbons, and pharmaceuticals. Under the general term of phytoremediation, several processes with distinctively different mechanisms of action are hidden. In this paper, the most popular modes of phytoremediation are described and discussed. A broad...
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Una egemonia instabile
Publikacjail ruolo degli Stati Uniti nell'economia globale e la sfida giapponese e cinese
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The New Chinese Civil Code and its contribution to Sustainable Development
PublikacjaThe first civil code of the People’s Republic of China in the history was adopted by the 13th National People’s Congress in Beijing on 28 May 2020 and will enter into effect on 1 January 2021. The new civil code puts much more emphasis on the sustainable development and protection of the environment and because of that, the Chinese private law has begun to respond to ecological problems as well. The...
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Influence of Honing Parameters on the Quality of the Machined Parts and Innovations in Honing Processes
PublikacjaThe article presents a literature review dealing with the effect of the honing parameters on the quality of the machined parts, as well as with the recent innovations in honing processes. First, an overview about the honing and the plateau-honing processes is presented, considering the main parameters that can be varied during machining. Then, the influence of the honing parameters on surface finish, shape deviation and material...
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Cellulose Nanomaterials in Biomedical, Food, and Nutraceutical Applications: A Review
PublikacjaNanotechnology with bionanomaterials have tremendous potential to enhance and utilize for nutrient and bioactive absorption, drug delivery systems, pharmaceutical, and nutraceutical field through various applications. Cellulose nanomaterials are green materials that are obtained from renewable sources and possess exceptional mechanical strength and biocompatibility. The associated unique physical and chemical properties have made...
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Quality of limes juices based on the aroma and antioxidant properties
PublikacjaKaffir (Citrus hystrix) and Key (Citrus aurantifolia) limes juices were investigated and compared. Two dimensional gas chromatography coupled with time-of-flight mass spectrometry (GC×GC-TOF-MS) was applied to assess the botanical origin of Kaffir and Key limes juices, based on volatile substances. The biggest differences in the contents of selected terpenes in Kaffir and Key limes occur in chemical compounds such as Limonene,...
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NADZOROWANIE WYPOSAŻENIA DO MONITOROWANIA I POMIARÓW WEDŁUG WYMAGAŃ WYBRANYCH NORM ORAZ PRZEPISÓW PRAWNYCH
Publikacja: Przyrządy pomiarowe stanowią zasadniczy element złożonego systemu oceny jakości wyrobów na wszystkich etapach produkcji. Odpowiednio zaprojektowane procedury opisujące procesy kontrolne i pomiarowe, sprawnie zorganizowane i przeprowadzane operacje monitorowania i pomiarów parametrów procesów i produktów oraz skutecznie funkcjonujący nadzór nad wyposażeniem do monitorowania i pomiarów w organizacji są podstawą do wykazania, że...
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Experimental and theoretical studies on the Sulfamethazine-Urea and Sulfamethizole-Urea solid-liquid equilibria
PublikacjaThe miscibility of active pharmaceutical ingredients with excipients is an important aspect in pharmaceutical technology protocols. In this study, the differential scanning calorimetry (DSC) was used for Sulfamethazine-Urea (SI–U) and Sulfamethizole-Urea (SO–U) solid-liquid phase diagrams determination. Both sulfonamides form simple binary eutectics with Urea. The lack of new co-crystal phase formation was confirmed by inspection...
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Effect of Glycemic Disorders and Habits on the Concentration of Selected Neurotrophic Factors in Patients with Lumbosacral Intervertebral Disc Degeneration
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QSRR Evaluation of the New Anticancer Sulfonamides in View of the cis-trans Isomerism
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Biological Activity of Compounds Exhibiting Local Anesthetics's Properties Evaluated by QSAR Approach
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Effect of Silicone on the Collagen Fibrillogenesis and Stability
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Function and Frustration of Multi-Drug ABC Exporter Protein and Design of Model Proteins for Drug Delivery Using Protein Hydration Thermodynamics
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Future of Protease Activity Assays
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Editorial(Hot Topic: Proteolysis in Health and Disease)
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Synthesis of isomeric, oxathiolone fuded chalcones and comparison of their activity toward various microorganisms and human cancer cell lines
PublikacjaIzomeryczne oksationolowe sprzężone chalkony otrzymano w wyniku kondensacji odpowiedniego acetylobenzo[1,3]oksatiolo-2-onu z aldehydem benzoesowym w środowisku kwaśnym. Określono aktywność cytotoksyczną otrzymanych związków wobec komórek linii HeLa, przeciwbakteryjną wobec Micrococcus luteus, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli i Proteus vulgaris, przeciwgrzybową wobec Candida albicans i tuberkulostatyczną...
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Comprehensive Spectroscopic Characterization of Finasteride Polymorphic Forms. Does the Form X Exist?
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Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate
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Substrate Reduction Therapies for Mucopolysaccharidoses
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pH-Induced modification to stratum corneum lipids investigated using thermal, spectroscopic, and chromatographic techniques
PublikacjaZbadano jakim zmianom jakościowym i ilościowym ulegają indywidualne klasy lipidów w Stratum Corneum (tkanka rogowa skóry) pod wpływem środowiska o zmiennym pH.
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Electrochemical and in silico approaches for liver metabolic oxidation of antitumor-active triazoloacridinone C -1305
Publikacja5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) is a promising antitumor compound developed in our laboratory. A better understanding of its metabolic transformations is still needed to explain the multidirectional mechanism of pharmacological action of triazoloacridinone derivatives at all. Thus, the aim of the current work was to predict oxidative pathways of C-1305 that would reflect its phase I metabolism. The...
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Modulation of cellular response to anticancer treatment by caffeine:inhibition of cell cycle checkpoints, DNA repair and more
PublikacjaKofeina i inne metyloksantyny wywołują bardzo różne efekty fizjologiczne w organizmie człowieka. W pracy przedstawiamy, które z tych efektów mogą wpływać na skuteczność terapii przeciwnowotworowych. Kofeina może bezpośrednio wpływać na transport oraz aktywację metaboliczną cząsteczek leków do komórki, poprzez tworzenie kompleksów z lekami zawierającymi układy poliaromatyczne. Kofeina hamuje aktywność kinaz ATM/ATR co prowadzi do...
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The Role of FLT3 Kinase as an AML Therapy Target
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Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublikacjaUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
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Prediction of Bioactive Peptides From Chicken Feather and Pig Hair Keratins Using In Silico Analysis Based on Fragmentomic Approach
PublikacjaBackground: Keratin is among the most abundant structural proteins of animal origin, however it remains broadly underutilized. Objective: Bioinformatic investigation was performed to evaluate selected keratins originating from mass-produced waste products, i.e., chicken feathers and pig hair, as potential sources of bioactive peptides. Methods: Pepsin, trypsin, chymotrypsin, papain, and subtilisin were used for in silico keratinolysis...
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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...