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Search results for: MULTI-SUBSTRATE ENZYME
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublicationZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublicationHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublicationIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublicationThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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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
PublicationIn 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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Electrochemical performance of thin free-standing boron-doped diamond nanosheet electrodes
PublicationIn the following work we describe preparation and the electrochemical performance of thin and free-standing heavy boron-doped diamond (BDD) nanosheets. The investigated foils were deposited on Ta substrate using microwave plasma-enhanced chemical vapor deposition technique (MPECVD). Foils of two B-dopant densities were investigated, obtained on the base of 10 k and 20 k ppm [B]/[C] ratio in the gas admixture. The obtained foils...
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Stratification of nano-pigments in anti-corrosive coatings by means of magnetic field
PublicationThe concept of self-stratification of coatings, although attractive, causes difficulties in its practical use, especially when pigments are added to the resins. An alternative way of obtaining a multilayer structure in a single step was presented. Using the inhomogeneous magnetic field and magnetically active components of the coating, the possibility of vertically graded differentiation of the one layer properties has been verified....
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Heat Transfer of the Multicolor-Laser-Sources-Irradiated Nanoparticles in Reference to Thermal Processes
PublicationUnlike the standard materials, metallic nanoparticles offer enhancing the heat convertion rate which implies the maximum and average temperature boost significantly in the considered system. The work’s purpose is to examine heat transfer in the metallic nanoparticles which have been deposited on a glassy substrate, enabling the nanostructures thermoablation. Furthermore, the functionalized substrate is irradiated with multicolor-laser-sources,...
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Comparison of experimental results with simulation studies of "digital" hydrostatic transmission
PublicationThe publication presents the results of experimental research on a "digital" hydrostatic transmission conducted at INOE 2000 IHP within the framework of the grant "Method of effective use of the digital hydraulics concept in multi-source hydrostatic drive systems". The primary goal of the research is to compare the effectiveness (efficiency) of using different methods of controlling the pump capacity and the hydraulic motor capacity...
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublicationA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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A higher order shell element for wave propagation in isotropic shell structures
PublicationThe presents the new multi mode higher order shell element for wave propagation problems in shell structures.
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Distributed Evolutionary Algorithm for Path Planning in Navigation Situation
PublicationThis article presents the use of a multi-population distributed evolutionary algorithm for path planning in navigation situation. The algorithm used is with partially exchanged population and migration between independently evolving populations. In this paper a comparison between a multi-population and a classic single-population algorithm takes place. The impact on the ultimate solution has been researched. It was shown that using...
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Consolidating logs in varying formats into a structured repository = konsolidacja logów w zmiennych formatach do strukturalnego repozytorium
PublicationDuring multi-agent systems development, testing and re- search, possibly voluminous logs are created at distributed agent loca-tions. These logs describe individual agents behavior and state changes. To get the complete picture of the multi-agent system working, it is necessary to consolidate these logs and to store them in a format appropriate for diverse analyzes. Specic issues arise during consolidation if the log formats are...
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The New LM-PCR/Shifter Method for the Genotyping of Microorganism
PublicationTechniques relies on the ligation of appropriates adapters (LM-PCR) as AFLP, PCR MP and ADSRRS are successfully used for epidemiological studies for prokaryotic and eukaryotic microorganisms. In this study we propose a new method, called the LM-PCR/Shifter, based on the use of a Class IIS restriction enzyme giving restriction fragments with different 4 base 5' overhangs (Shifter) and the ligation of appropriate oligonucleotide...
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A Novel Cryptic Clostridial Peptide That Kills Bacteria by a Cell Membrane Permeabilization Mechanism
PublicationThis work reports detailed characteristics of the antimicrobial peptide Intestinalin (P30), which is derived from the LysC enzyme of Clostridium intestinale strain URNW. The peptide shows a broader antibacterial spectrum than the parental enzyme, showing potent antimicrobial activity against clinical strains of Gram-positive staphylococci and Gram-negative pathogens and causing between 3.04 ± 0.12 log kill for Pseudomonas aeruginosa...
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Targeting Spike‐ACE2 Interface of SARS‐CoV‐2 and its Omicron Variant: A Comparative Screening of Potential Inhibitors for Existing and Anticipating Variants Using Molecular Modelling Approach
PublicationThe recent COVID pandemic has shown major impact on public health and economic crisis. Despite the development of many vaccines and drugs against the severe acute respiratory syndrome (SARS) coronavirus 2, the pandemic still persists. The continued spread of the virus is largely driven by the emergence of viral variants such as α, β, γ, delta, epsilon spike, omicron and its subvariants (BA.1,2,3) which can evade the current vaccines...
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Thermally tuneable optical and electrochemical properties of Au-Cu nanomosaic formed over the host titanium dimples
PublicationAu-Cu nanostructures offer unique optical and catalytic properties unlike the monometallic ones resulting from the specific interaction. Among others, they have the ability to exhibit surface plasmon resonance, electrochemical activity towards the oxygen and hydrogen evolution reaction (OER, HER) as well as improved photoresponse in relation to monometalic but those properties depend highly on the substrate where bimetallic structures...
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Extending the Frequency Limit of Microstrip-Coupled CSRR Using Asymmetry
PublicationAbstract— This article explains the frequency limitation in designing microstrip circuits based on a complementary split-ring resonator (CSRR) and reports a novel technique for increasing its operating frequency, which makes the CSRR suitable for high-frequency applications. This study helps in synthesizing the dimensions of symmetric CSRR (SCSRR) and asymmetric CSRR (ACSRR) circuits, which shows the applicability of the proposed...
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Electrophoretic deposition and characterization of composite chitosan/Eudragit E 100 or poly(4-vinylpyridine)/mesoporous bioactive glass nanoparticles coatings on pre-treated titanium for implant applications
PublicationTitanium implants are surface-modified to achieve bioactivity and often antibacterial properties. Such surface coatings may increase corrosion degradation and be weakly attached to the substrate. In the present research, biodegradable composite coatings, investigated so far as smart environment-sensitive, slowly releasing silver to the implant neighborhood, were produced as a combination of chitosan (CS) with Eudragit E 100 (EE100)...
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Sensorless control of five-phase induction machine supplied by the VSI with output filter
PublicationIn this paper, a novel sensorless control structure based on multi-scalar variables is proposed. The tatic feedback control law is obtained by using the multi-scalar variables transformation, where the multi-scalar variables approach allows a full linearization of the nonlinear system. The control system could be described as “optimized” because of the minimized number of controllers. Furthermore, control system is divided into...
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A novel sensor for measuring temperature profile during the thermoablation
PublicationAbstract — A novel approach for monitoring a temperature distribution inside a tissue during thermoablation is presented in the paper. A thermal profile is measured using a set of serially connected thermistors each bypassed by a capacitor. This technique allows a two-wire and simultaneous multi- point measurements using a multi-frequency measurement of electrical impedance. It is...
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SAILING ROUTE PLANNING METHOD CONSIDERING VARIOUS USER CATEGORIES
PublicationThe article describes the methodology related to determining the multi-criteria routes for sailing ships. Details of sea area discretisation and discretisation of the description of the sailing vessel properties and manoeuvring principles are shown. User requirements were specified (for five different categories of users) and on this basis the criteria for selecting the most suitable shipping route were formulated. The presented...
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DDLMS PCR double digestion Ligation Mediated Suppression PCR - a new technique for bacterial specific differentiation
PublicationA new diagnostic kit for K. oxytoca specific differentiation based on ddLMS PCR (ang. double digest ligation Mediated PCR) technique is shown. As a species-specific DNA fragment pehX gene, encoding the enzyme polygalactouronase, was chosen. The genome sequence of K. oxytoca is digested with two endonucleases: AclI and BclI which cut DNA before and after pehX gene. The polymorphic DNA fragments are ligated with AclI-end-specific...
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Removal of persistant organic pollutants from landfill leachates treated in three constructed wetland systems
PublicationThe objective of the study was assessment of occurrence and removal of two groups of persistent organic pollutants: polycyclic aromatic hydrocarbons (PAHs) and polychlorinated biphenyls (PCBs) in landfill leachate (LL) treated in three constructed wetland systems (CWs) of different construction and flow regime. Two subsurface flow systems (SSF) were analyzed: one with horizontal flow and the second one consisting of two vertical...
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Application of Vertical Reed Beds as a Buffer for Effluent from SBR ANAMMOX Treatment for Reject Water from Centrifugation
PublicationThe main purpose of this study is to determine the removal efficiency of nitrogen compounds in the effluentfrom ANAMMOX process used to treat reject water after centrifugation. A pilot model was bulit consisting of fourdifferent Treatment Wetlands beds with different filter substrate and with or without macrophytes growth. Verticalsubsurface flow type filters have been choosen thanks to their highest efficiency in NH4-N removal...
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Scoreboard Architectural Pattern and Integration of Emotion Recognition Results
PublicationThis paper proposes a new design pattern, named Scoreboard , dedicated for applications solving complex, multi-stage, non-deterministic problems. The pattern provides a computational framework for the design and implementation of systems that integrate a large number of diverse specialized modules that may vary in accuracy, solution level, and modality. The Scoreboard is an extension of Blackboard design pattern and comes under...
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An Analysis of Elliptical-Rectangular Patch Structure on Multilayer Elliptic Cylinders
PublicationThe resonance frequency problem of an ellipticalrectangular patch mounted on multilayered dielectric coated elliptic conducting cylinder, is investigated in this paper. A fullwave analysis and a moment-method calculation are employed. The analysis is carried out considering the expansion of the field as a series of Mathieu functions. An additional theorem for Mathieu functions is utilized to investigate the non-confocal ellipse...
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Accurate modeling of layout parasitic to forecast EMI emitted from a DC-DC converter.
PublicationThis paper illustrates how to account for all parasitic due to the layout of a power converter (inductive and capacitive), in order to forecast electromagnetic interferences (EMI). The method is generic, and is validated here in the simple example of a DC-DC converter, realized on different technologies: insulated metal substrate (IMS), printed circuit board (PCB). In addition, several layouts aspects will be investigated. Conclusions...
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Jahn-Teller and related conical intersections in the benzene radical cation and the monofluoro derivate
PublicationThe multi-state multi-mode vibronic interactions in the benzene radical cation and its monofluoro derivative have been investigated theoretically, based on high-level electronic structure calculations for the system parameters and a quantum treatment of the nuclear motion. The available experimental data are well reproduced. The interplay of different vibronic coupling mechanisms is pointed out leading to multiple nonadiabatic...
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Revisiting Supervision for Continual Representation Learning
Publication"In the field of continual learning, models are designed to learn tasks one after the other. While most research has centered on supervised continual learning, there is a growing interest in unsupervised continual learning, which makes use of the vast amounts of unlabeled data. Recent studies have highlighted the strengths of unsupervised methods, particularly self-supervised learning, in providing robust representations. The improved...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublicationStructures 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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Recent advances in high-frequency modeling by means of domain confinement and nested kriging
PublicationDevelopment of modern high-frequency components and circuits is heavily based on full-wave electromagnetic (EM) simulation tools. Some phenomena, although important from the point of view of the system performance, e.g., EM cross-coupling effects, feed radiation in antenna arrays, substrate anisotropy, cannot be adequately accounted for using simpler means such as equivalent network representations. Consequently, the involvement...
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Expedited Yield-Driven Design of High-Frequency Structures by Kriging Surrogates in Confined Domains
PublicationUncertainty quantification is an important aspect of engineering design, also pertaining to the development and performance evaluation of high-frequency structures systems. Manufacturing tolerances as well as other types of uncertainties, related to material parameters (e.g., substrate permittivity) or operating conditions (e.g., bending) may affect the characteristics of antennas or microwave devices. For example, in the case...
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Seeding enhancement for microcrystaline diamond layers growth on non-diamond substrates
PublicationThe present paper gives an overview on the possible methods of seeding substrates for diamond layers growth. Diamond in reason of his properties is very desirable material in microelectronic, biomedical and waste treatment sensors. Microcrystalline diamond for these applications must be grown on silicon substrate in microwave plasma assisted chemical vapor deposition (MPACVD). To grow diamond on non-diamond surface pre-growth...
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Growth and Isolation of Large Area Boron‐Doped Nanocrystalline Diamond Sheets: A Route toward Diamond‐on‐Graphene Heterojunction
PublicationMany material device applications would benefit from thin diamond coatings, but current growth techniques, such as chemical vapor deposition (CVD) or atomic layer deposition require high substrate and gas‐phase temperatures that would destroy the device being coated. The development of freestanding, thin boron‐doped diamond nanosheets grown on tantalum foil substrates via microwave plasma‐assisted CVD is reported. These diamond...
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The impact of slowly biodegradable organic compounds on the oxygen uptake rate in activated sludge systems
PublicationThe hydrolysis process of slowly biodegradable substrate (Xs) have impact on the efficiencies of nutrient removal in activated sludge systems. Measurement of OUR and corresponding COD is accepted as a very useful tool to reflect the consumption of biodegradable substrates. The influence of the readily biodegradable substrate (Ss) in biological wastewater treatment systems has been extensively investigated, but little is known about...
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The impact of slowly biodegradable organic compounds on the oxygen uptake rate in activated sludge systems
PublicationThe hydrolysis process of slowly biodegradable substrate (Xs) have impact on the efficiencies of nutrient removal in activated sludge systems. Measurement of OUR and corresponding COD is accepted as a very useful tool to reflect the consumption of biodegradable substrates. The influence of the readily biodegradable substrate (Ss) in biological wastewater treatment systems has been extensively investigated, but little is known about...
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Design and Optimization of Metamaterial-Based 5G Millimeter Wave Antenna for Gain Enhancement
PublicationIn this brief, a low profile, broadband, high-gain antenna array based on optimized metamaterials (MMs) with dual-beam radiation is reported for 5G millimeters wave (mm-wave) applications. The design is a simple bow tie operating at a 5G band of 28 GHz. It consists of two bow ties with substrate integrated waveguide (SIW)-based power splitter. A broad impedance bandwidth of 26.3−29.8 GHz is obtained by appropriately combining the...
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Low-strain sensor based on the flexible boron-doped diamond-polymer structures
PublicationA free-standing high boron-doped diamond nanosheet (BDDNS) has been fabricated for the development of a flexible BDDNS strain senor. High boron-doped diamond was initially grown on a tantalum substrate in a microwave plasma-assisted chemical vapor deposition method, and was then transferred to a Kapton polymer substrate to fabricate the flexible BDDNS/Kapton device. Before performing the transfer process, the thin BDDNS’s morphology...
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Study of Nanohydroxyapatite Coatings Prepared by the Electrophoretic Deposition Method at Various Voltage and Time Parameters
PublicationThe aim of the work is to compare the properties of nanohydroxyapatite coatings obtained using the electrophoretic deposition method (EDP) at 10 V, 20 V, and 30 V, and with deposit times of 2 and 5 min. The primary sedimentation was used to minimize the risk of the formation of particle agglomerates on the sample surface. Evaluation of the coating was performed by using a Scanning Electron Microscope (SEM), Energy-Dispersive Spectroscopy...
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Model of management of knowledge bases in the information technology evaluation environment
PublicationThe paper presents the model of management of knowledge bases in multi-agent system for evaluation of information technologies (IT_MAS). Such system is being developed in Gdansk Uni-versity of Technology by Information Technology Management Team. Multi-agent system is supposed to support manager level specialists during decision processes when there is identified need to buy or change any information technology. The main goal of...
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DYNWIR S-70 program for modal analysis of multisupported and multimass rotors
PublicationThe article provides a brief description of the program Dynwir-S-70 (currently being developed in the Rotor Dynamics and Slide Bearings Department in the Institute of Fluid-Flow Machinery Polish Academy of Sciences in Gdansk) which is a program for analysis of multi-supported and multi-mass rotors. Used algorithms and the construction of mass and stiffness matrix were presented. Damping matrix structure based on Rayleigh damping...
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Comparative Greenness Evaluation
PublicationGreenness of analytical procedure is multivariable aspect as many greenness criteria should be taken into consideration. On the other hand, modern analytical chemistry offers dozens of analytical procedures, based on different sample preparation and final determination techniques that are used for the determination of a given analyte in a given matrix. For such complex decision-making processes, multi-criteria decision analysis...