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Wyniki wyszukiwania dla: BISPHENOL A ANALOGUES
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Synthesis and antimicrobial activity of truncated fragments and analogs of citropin 1.1: The solution structure of the SDS micelle-bound citropin-like peptides
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Antiproliferative activity of side-chain truncated vitamin D analogs (PRI-1203 and PRI-1204) against human malignant melanoma cell lines
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NMR studies of new arginine vasopressin analogs modified with α-2-indanylglycine enantiomers at position 2 bound to sodium dodecyl sulfate micelles
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublikacjaIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Determination of Hydroxy Groups in the Modified Epoxy Oligomers Using IR-Spectroscopy
PublikacjaThe use of IR-spectroscopy has been proposed to determine the content of hydroxy groups in the modified functional oligomers based on bisphenol A diglycidyl ether. Apart from hydroxy groups the investigated oligomers contain epoxy or peroxy, carboxy or acrylic groups.
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Distributed Representations Based on Geometric Algebra: the Continuous Model
PublikacjaAuthors revise the concept of a distributed representation of data as well as two previously developed models: Holographic Reduced Representation (HRR) and Binary Spatter Codes (BSC). A Geometric Analogue (GAc - ''c'' stands for continuous as opposed to its discrete version) of HRR is introduced - it employs role-filler binding based on geometric products. Atomic objects are real-valued vectors in n-dimensional Euclidean space...
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Analytical aspects of model compounds toxicity assessment using MTT and Microtox bioanalytica assays
PublikacjaMore and more increased intensity of anthropopressure processes can be observed, among other things, in the release of great quantities of synthetic substances into the environment, including the Endocrine Disrupting Compounds. The effects of the above-mentioned human impact on the environment not only can be noticed in the homeostasis disturbance in ecosystems, but they are also visible with respect to human. The high incidence...
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublikacjaSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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Ionic liquids as an effective and eco-friendly medium for synthesis of nitrosubstituted norbornene analogs Ciecze jonowe jako efektywne i przyjazne środowisku medium dla syntezy nitropodstawionych analogów norbornenu
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Simple and novel synthesis of 3-(thio)phosphoryl-β-lactams by radical cyclization
PublikacjaRadical cyclization of phosphono-acetenamides promoted by manganese(III) acetate leads exclusively to the formation of 3-phosphoryl-β-lactams. The thiophosphoryl analogues were also prepared using this method. In particular, the presented protocol does not require the use of noble metals, while comparable methods do.
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Programmable Input Mode Instrumentation Amplifier Using Multiple Output Current Conveyors
PublikacjaIn this paper a programmable input mode instrumentation amplifier (IA) utilising second generation, multiple output current conveyors and transmission gates is presented. Its main advantage is the ability to choose a voltage or current mode of inputs by setting the voltage of two configuration nodes. The presented IA is prepared as an integrated circuit block to be used alone or as a sub-block in a microcontroller or in a field...
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Experimental and theoretical solubility advantage screening of bi-component solid curcumin formulations
PublikacjaA comprehensive experimental and theoretical screening was performed for identification of curcumin solubilizers. Experimental data led to formulation of a non-linear QSPR model correlating molecular descriptors with measured solubilities. The majority of synthesized binary systems exhibited a moderate enhancement of curcumin solubility, which was found to be the highest in the case of curcumin cocrystallized with pyrogallol. New...
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(CsX)Cu5O2(PO4)2 (X = Cl, Br, I): A Family of Cu2+ S = 1/2 Compounds with Capped-Kagomé Networks Composed of OCu4 Units
PublikacjaThree new salt inclusion compounds (CsX)Cu5O2(PO4)2 (X = Cl, Br, I), phosphate analogues of the kagomé mineral averievite, are reported. Their crystal structures are composed of trigonal networks of corner-sharing OCu4 anion-centered tetrahedra, forming capped-kagomé planes, which can also be regarded as two-dimensional slices along the [111] direction of a pyrochlore lattice. Magnetization and heat capacity measurements reveal...
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Ho2Pd1.3Ge2.7 – a ternary AlB2-type cluster glass system
PublikacjaWe report a successful synthesis of a ternary AlB2-type intermetallic compound. The phase purity was obtained by fine-tuning the Pd-Ge ratio out of the idealized 1-3. Attempts to synthesize an Er analogue were not successful. We discuss the instability of the Er analogue based on the atomic size ratio and also suggest that the increased stability of Ho2Pd1+xGe3−x in the Pd-rich range likely stems from a combination of atomic size...
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublikacjaNumerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methoxyfumaroyl)-L-2,3- diaminopropanoic acid (FMDP) has been extensively studied in order to develop its more active analogues. Several peptide−FMDP conjugates were tested to deliver FMDP to its...
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Characteristics of an image sensor with early-vision processing fabricated in standard 0.35 µm CMOS technology
PublikacjaThe article presents measurement results of prototype integrated circuits for acquisition and processing of images in real time. In order to verify a new concept of circuit solutions of analogue image processors, experimental integrated circuits were fabricated. The integrated circuits, designed in a standard 0.35 µm CMOS technology, contain the image sensor and analogue processors that perform low-level convolution-based image...
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Analog CMOS processor for early vision processing with highly reduced power consumption
PublikacjaA new approach to an analog ultra-low power visionchip design is presented. The prototype chip performs low-levelconvolutional image processing algorithms in real time. Thecircuit is implemented in 0.35 μm CMOS technology, contains64 x 64 SIMD matrix with embedded analogue processors APE(Analogue Processing Element). The photo-sensitive-matrix is of2.2 μm x 2.2 μm size, giving the density of 877 processors permm2. The matrix dissipates...
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Influence of Storage Time and Temperature on the Toxicity, Endocrine Potential, and Migration of Epoxy Resin Precursors in Extracts of Food Packaging Materials
PublikacjaThe aim of the present study was to establish a standard methodology for the extraction of epoxy resin precursors from several types of food packages (cans, multi-layered composite material, and cups) with selected simulation media (distilled water, 5% ethanol, 3% dimethyl sulfoxide, 5% acetic acid, artificial saliva) at different extraction times and temperatures (factors). Biological analyses were conducted to determine the acute...
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New conjugates of tuftsin and muramyl dipeptide as stimulators of human monocytes-derived dendritic cells
PublikacjaMuramyl dipeptide (MDP) and tuftsin are known biologically active compound displaying a significant influence on various cell populations of innate immune response. MDP, as a fragment of bacterial cell wall, stimulates not only macrophages and monocytes, but also dendritic cells. In contrast, little is known about tuftsin influence on these cells. Therefore it seemed vital to access whether tuftsin or its derivatives conjugated...
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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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Measurement method for capacitive sensors for microcontrollers based on a phase shifter
PublikacjaA complete measurement method dedicated to capacitive sensors has been developed. It includes the development of hardware (an analogue interface circuit for microcontrollers with built-in times/counters and analogue comparators) and software (a measurement procedure and a systematic error calibration (correction) algorithm which is based on a calibration dictionary). The interface circuit consists of a low-pass filter and a phase...
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Ultrasound assisted solvent extraction of porous membrane-packed samples followed by liquid chromatography-tandem mass spectrometry for determination of BADGE, BFDGE and their derivatives in packed vegetables
PublikacjaThe problem of the presence of trace organic pollutants in food is of growing importance due to increasing awareness about their impact on newborns, infants and adults of reproductive age. Despite the fact that packaged food products offer many advantages, packaging can be a source of contamination for stored food. Thus, monitoring such pollution in food is of high importance. In this work, a novel methodology based on the solvent...
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Selected organophosphorus compounds with biological activity. Applications in medicine
PublikacjaThe purpose of this article is to provide an overview of the latest applications of organophosphorus compounds (OPs) that exhibit biological activity. A large family of OPs have become popular in recent years. The practical application of OPs in modern medicine has been attributed to their unique properties. In this article, the methods used to select these compounds will be emphasized. This paper will first outline the findings...
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Fracture of aluminium joints bonded with epoxy adhesive reinforced by mmt nanoparticles
PublikacjaCrack propagation behavior was studied for aluminium/aluminum adhesive joints bonded with two epoxy adhesives: pure and reinforced with clay nanoparticles. The focus was also on the novel use of the constant displacement rate test to study adhesion/adhesives efficiency. The epoxy systems studied were: Epidian E6 produced from bisphenol A and epichlorohydrin, (''Organika -Sarzyna'' Poland); pure or strengthened with montmorillonit...
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A novel (Ti/Ce)UiO-X MOFs@TiO2 heterojunction for enhanced photocatalytic performance: Boosting via Ce4+/Ce3+ and Ti4+/Ti3+ redox mediators
PublikacjaTitanium-substituted cerium-oxo-based UiO MOFs with terephthalate linkers modified by various groups (–Br, –NH2, –NO2) or their derivatives (N-heterocyclic or biphenyl groups) were combined with titanium dioxide in a multistep route to obtain a core-shell-like architecture. DFT simulations showed that Ce- and bimetallic Ti/Ce- MOFs exhibited different charge compensation. Extended characterization revealed the formation of heterojunctions between...
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Experiments on Preserving Pieces of Information in a Given Order in Holographic Reduced Representations and the Continuous Geometric Algebra Model
PublikacjaGeometric Analogues of Holographic Reduced Representations (GAc, which is the continuous version of the previously developed discrete GA model) employ role-filler binding based on geometric products.Atomic objects are real-valued vectors in n-dimensional Euclidean space and complex statements belong to a hierarchy of multivectors. The property of GAc and HRR studied here is the ability to store pieces of information in a given...
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Synthesis and biological evaluation of N-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) is responsible for the hydrolysis of biologically inactive sulfated steroids into their active un-sulfated forms and promotes the growth of various hormone-dependent cancers (e.g., breast cancer). Therefore, the STS enzyme is a promising therapeutic target for the treatment of steroid-sensitive cancers. Herein, we report the synthesis and biological evaluation of sulfamate analogs as potential STS inhibitors...
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Obtaining of Coumarone-Indene Resins Based on Light Fraction of Coal Tar. 4. Bitumen-Polymer Blends with Participation of Coumarone-Indene Resins with Epoxy Groups
PublikacjaUsing light fraction of coal tar (5.75 wt % of coumarone and 44.45 wt % of indene), glycidyl methacrylate and styrene, the coumarone-indene resin with epoxy groups (CIRE) has been synthesized. Monoperoxy derivative of diglycidyl ether Bisphenol A (PO) was used as an initiator. The possible formation of CIRE has been studied on the model systems consisting of PO, glycidyl methacrylate, indene or coumarone, or styrene, or mixture...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublikacjaMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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Digital Control System of the Wavemaker in the Towing Tank
PublikacjaThe paper describes a digital control system of the rigid flap wavemaker in a towing tank in CTO S.A. Ship Design and Research Centre. The control system is based on an 8-bit AVR microcontroller and consists of two cascading PID controllers. The digital system replaced the previous analogue system from 1974 and has been integrated with the existing sensors and actuators of the wavemaker. The new control system allows to obtain...
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Words context analysis for improvement of information retrieval
PublikacjaIn the article we present an approach to improvement of retrieval informationfrom large text collections using words context vectors. The vectorshave been created analyzing English Wikipedia with Hyperspace Analogue to Language model of words similarity. For test phrases we evaluate retrieval with direct user queries as well as retrieval with context vectors of these queries. The results indicate that the proposed method can not...
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Selected Methods for the Chemical Phosphorylation and Thiophosphorylation of Phenols
PublikacjaThis Focus Review gathers together a selection of methods for the chemical phosphorylation of phenols that employ three‐ and four‐coordinate phosphorus compounds. Phosphorylated scaffolds can exhibit enhanced properties compared to their non‐phosphorylated analogues, such as increased biological activity and increased/decreased solubility; as such, phosphorus compounds have gained more and more interest in organic and medicinal...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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Exploring the Reactivity of Unsymmetrical Diphosphanes toward Heterocumulenes: Access to Phosphanyl and Phosphoryl Derivatives of Amides, Imines, and Iminoamides
PublikacjaWe present a comprehensive study on the diphosphanation of iso(thio)cyanates by unsymmetrical diphosphanes. The reactions involving unsymmetrical diphosphanes and phenyl isocyanate or phenyl thioisocyanate gave rise to phosphanyl, phosphoryl, and thiophosphoryl derivatives of amides, imines, and iminoamides. The structures of the diphosphanation products were confirmed through NMR spectroscopy, IR spectroscopy, and single-crystal...
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Negative thermal expansion and antiferromagnetism in the actinide oxypnictide NpFeAsO
PublikacjaPrzeprowadzona został udana synteza NpFeAsO, związku będącego analogiem do LaFeAsO. Stwierdzono występowanie antyferromagnetycznego uporządkowania z T_N = 57 K. Poniżej T_N zauważono tzw. ujemną rozszerzalność termiczną. Przeprowadzono badania dyfrakcyjne przy użyciu promieniowania synchrotronowego (ESRF - Grenoble) a także neutronów (ILL - Grenoble).
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Zero phase shift digital filtering for assessment of exposure to non-sinusoidal magnetic fields
PublikacjaAccuracy of assessment of human body exposure to magnetic fields is affected by several uncertainty sources. One of them is estimation of the total exposure to non-sinusoidal fields. Standard methods can be implemented using analogue or digital filters that introduce a phase shift that affect the result of total exposure level estimation. The paper presents a new method that allows performing more precise assessment of exposure...
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An insight into craft activities in rural areas of Dalmatia province - first data on iron working at the Roman settlement in Lopar (Island of Rab)
PublikacjaWithin multidisciplinary research carried out at Podšilo bay in Lopar on the island of Rab (north-eastern Adriatic), on the bases of movable finds and, possibly, geophysical measurements, evidence of ironworking has been detected within a Roman rural site where ceramic building materials production was ascertained before. Preliminary analyses of several samples of slug, iron objects and nearby collected minerals support the...
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Pharmaceutical applications of surfactants
PublikacjaIn this study we focused on biological activity of various surfactants. According to our research, they con act both as carriers as well as therapeutic agents. Depending on their concentration, they can create different structures in a solution, which influence their properties. Liposomes have a significant role in drug delivery system. Surfactants in from of bilayer are analogous to natural biological cell membrane.
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Histaminol and Its Complexes with Copper(II) - Studies in Solid State and Solution
PublikacjaHistaminol [4(5)-(B-hydroxyethyl)imidazole, 4-(1H-imidazol-2-yl)ethanol, L] is an analogue of histamine and its minor metabolite. So far its properties have not been studied in detail due to the synthetic difficulties. Here, the structure and acid-base properties of histaminol, as well as the results of studies on its copper(II) complexes in solid state and aqueous solution are reported. Stability constants of the histaminol–CuII...
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Stabilizacja w gruncie
PublikacjaSpecyficzne zachowania gruntu w strefach przyległych do kanalizacyjnych studzienek rewizyjnych (komór przepompowni ścieków itp.). Stabilizacja położenia jako efekt niewłaściwego postępowania w fazie robót budowlano - montażowych, w tym zasypki obiektów. Różnice i analogie dla konstrukcji "sztywnych" i "elastycznych".
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Nowe substancje psychoaktywne. Cz. I. Współczesna sytuacja narkotykowa
PublikacjaGwałtowny wzrost liczby substancji wprowadzanych na rynek narkotykowy został zaobserwowany już pod koniec lat dziewięćdziesiątych XX wieku. Każdego roku syntezowane są nowe substancje jako analogi już istniejących, a ich ilość systematycznie rośnie. Niejednokrotnie wprowadzenie niewielkiej zmiany w strukturze związku może spowodować znaczne zmiany ich właściwości fizykochemicznych oraz psychoaktywnych. Nowe substancje psychoaktywne...
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Provenance studies on Late Neolithic amber ornaments from North-East Poland
PublikacjaThe area of North-East Poland was in prehistory, and still is today, an area with easy access to amber as a raw material, as is evidenced in part by numerous Late Neolithic (3rd millennium) amber workshops located in the Gulf of Gdańsk and Żuławy Wiślane (Vistula Fens). Given this fact, it is surprising that only a few finished amber products have been recovered from this area. Among them are unique ornaments from the Late Neolithic...
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Bell-Type Inequalities from the Perspective of Non-Newtonian Calculus
PublikacjaA class of quantum probabilities is reformulated in terms of non-Newtonian calculus and projective arithmetic. The model generalizes spin-1/2 singlet state probabilities discussed in Czachor (Acta Physica Polonica:139 70–83, 2021) to arbitrary spins s. For s → ∞ the formalism reduces to ordinary arithmetic and calculus. Accordingly, the limit “non-Newtonian to Newtonian” becomes analogous to the classical limit of a quantum theory
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Symulacje habitatów marsjańskich.
PublikacjaW pierwszych misjach załogowych na Marsa ludzie będą mieszkać w prostych metalowych modułach. Ich gabaryty i masa będą niewielkie ze względu na ograniczone możliwości rakiet wynoszących. W programie MARS (Mars Analogue Research Station) zorganizowanym przez stowarzyszenie Mars Society prowadzi się symulacje życia i pracy przyszłych marsonautów. Pomaga to m. in. w ozptymalizowaniu układu funkcjonalnego w module. Trwają poszukiwania...
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Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublikacjaGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
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ELECTRON ATTACHMENT TO HETEROGENEOUS MOLECULAR CLUSTERS
PublikacjaHeterogeneous clusters are unique model species enabling studies of bulk and surface processes by vacuum restricted methods. This is of particular importance for the reactions of low-energy electrons which have extremely short penetration depth in bulk environments. This contribution overviews our recent experiments with low-energy electrons and clusters prepared by different techniques. First, the deposition of molecules on argon...
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Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
PublikacjaThe aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant,...
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Preliminary typology and contextual analysis of Roman and late antique cooking wares from the Roman rural settlement at Podšilo bay on the island of Rab (north–eastern Adriatic, Croatia)
PublikacjaThe paper presents a preliminary typology of coarse cooking ware from the Roman/late antique layers of the rural settlement at Podšilo bay on the island of Rab. The vessels have been associated with several basic shapes and divided by types, while fabrics have been described macroscopically. Analogies and a contextual analysis were used to propose dating and to assess provenience for well-known ware classes or to define areas...