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Glutamine analogues containing a keto function - novel inhibitors of fungal glucosamine-6-phosphate synthase
PublikacjaW publikacji przedstawiono syntezę nowych pochodnych kwasu (S)-2,3-diaminopropanowego, zawierających reszty kwasów z funkcją ketonową. Dla otrzymanych związków zbadano właściwości inhibicyjne w stosunku do grzybowej syntazy glukozamino-6-fosforanu, ustalono właściwości lipofilowe otrzymanych związków a także aktywność przeciwgrzybową. Dla kilku wybranych pochodnych otrzymano ich dipeptydy, zbadano także ich aktywność przeciwgrzybową...
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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublikacjaDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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The biological role of prolyl oligopeptidase and the procognitive potential of its peptidic inhibitors from food proteins
PublikacjaProlyl oligopeptidase (POP) is a conserved serine protease belonging to proline-specific peptidases. It has both enzymatic and non-enzymatic activity and is involved in numerous biological processes in the human body, playing a role in e.g., cellular growth and differentiation, inflammation, as well as the development of some neurodegenerative and neuropsychiatric disorders. This article describes the physiological and pathological...
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Structure–activity relationships study on biological activity of peptides as dipeptidyl peptidase IV inhibitors by chemometric modeling
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Inhibitors and Antibody Fragments as Potential Anti-Inflammatory Therapeutics Targeting Neutrophil Proteinase 3 in Human Disease
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Design of serine proteinase inhibitors by combinatorial chemistry using trypsin inhibitor SFTI‐1 as a starting structure
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Development of Biocompatible Fe3O4@SiO2 Nanoparticles as Subcellular Delivery Platform for Glucosamine-6-phosphate Synthase Inhibitors
PublikacjaNumerous inhibitors of glucoseamine-6-phophate synthase (GlcN-6-P), the enzyme responsible from catalysis of the first step of metabolic pathway leading to metabolism 5’-diphospho-N-acetyl-D- glucosamine, were reported as effective agents for inhibiting the growth of various fungal pathogens. Among the reported inhibitors,...
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Structure-activity relationship study of tetrapeptide inhibitors of the Vascular Endothelial Growth Factor A binding to Neuropilin-1
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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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LY294002 and sorafenib as inhibitors of intracellular survival pathways in the elimination of human glioma cells by programmed cell death
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Synthesis and biological evaluation of fluorinated 3-phenylcoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
PublikacjaIn the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect in the enzymatic...
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Taq DNA polymerase fused with DNA binding protein with increased resistance to inhibitors from clinical samples
PublikacjaNowadays PCR method is commonly used in molecular diagnostic. However, in many cases PCR is limited, by the presence of inhibitory substances in biological, soil or food samples Efficiency and fidelity of amplification is strongly connected with DNA polymerase and reaction conditions. To meet the requirements of modern diagnostic methods it is essential to seeking for new DNA polymerases with better properties useful in these field....
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublikacjaResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Effect of selected ammonia escape inhibitors on carbon dioxide capture and utilization via calcium carbonate precipitation
PublikacjaCarbon dioxide was used to precipitate CaCO3 with CaCl2 solution in the presence of NH3 as a CO2 absorption promoter. Compounds that were previously indicated as inhibitors of ammonia escape during CO2 absorption were also added to the reaction mixture. Inorganic salts, i.e. ZnCl2, CuCl2, CoCl2, and organic substances, i.e. glycerol, ethylene glycol and triethanolamine were tested inhibitors in this work. A model post-distillation...
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Chloroacridine derivatives as potential anticancer agents which may act as tricarboxylic acid cycle enzyme inhibitors
PublikacjaThe chloroacridines affect biological forms of melanoma in different ways. Amelanotic (Ab) melanoma (with inhibited melanogenesis and higher malignancy) was particularly sensitive to the action of the chloroacridines. The Ab melanoma cells died through apoptosis and through death without caspase activation. Diminished activity of TAC enzymes was noticed among Ab melanoma cells together with ATP/NAD depletion, especially in the...
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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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The Distribution of Glucosinolates in Different Phenotypes of Lepidium peruvianum and Their Role as Acetyl- and Butyrylcholinesterase Inhibitors—In Silico and In Vitro Studies
PublikacjaThe aim of the study was to present the fingerprint of different Lepidium peruvianum tu- ber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform)....
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Design of new cholinesterase inhibitors based on phosphorus analogs of tacrine as potential anti-Alzheimer’s disease agents
PublikacjaBased on the analysis of the determined free binding energy (using the AutoDock Vina 1.1.2 docking program), the most potent cholinesterase inhibitors were selected. Moreover, studies of 3D visualization of the results of molecular modeling led to the identification of potential sites for the interaction of new potential inhibitors with amino acid residues building active sites of investigated cholinesterases.
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Experimental investigation of domestic micro-CHP based on the gas boiler fitted with ORC module
PublikacjaThe results of investigations conducted on the prototype of vapour driven micro-CHP unit integrated with a gas boiler are presented. The system enables cogeneration of heat and electric energy to cover the energy demand of household. The idea of such system is to produce electricity for own demand or for selling it to the electric grid – in such situation the system user will became the prosumer. A typical commercial gas boiler,...
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Experimental ORC micro-power plant for CHP application Part A: power plant arrangement
PublikacjaThe co-generative micro-power plant with the HFE7100 applied as a working medium was designed and built for experimental investigations. The heat output of the plant was assumed equal to 20 kW, while the electric output amounted to about 3kW. Examples of the results of the preliminary experimental research on a boiler, heat exchangers, a pump and a turbine-generator set are presented and analysed.
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Increase of power and efficiency of the 900 MW supercritical power plant through incorporation of the ORC
PublikacjaThe objective of the paper is to analyse thermodynamical and operational parameters of the supercritical power plant with reference conditions as well as following the introduction of the hybrid system incorporating ORC. In ORC the upper heat source is a stream of hot water from the system of heat recovery having temperature of 90 °C, which is additionally aided by heat from the bleeds of the steam turbine. Thermodynamical analysis...
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Operation of the 900 MW power plant with the ORC supplied from three heat sources
PublikacjaThe chapter is aimed at utilisation of waste heat in the reference supercritical power plant in the manner to produce electricity in ORC installation. The waste heat is available in the form of a stream of hot water at 90°C, recovered from the exhaust gases in the amount of 200MW. Such low enthalpy heat source is rather insufficient to produce a good quality vapour to feed the ORC turbine. Therefore an original approach to increase...
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RAPORT - EKSPERTYZA Z POMIARÓW DRGAŃ LINII WAŁÓW NA JEDNOSTCE ORP „DĄBIE”
PublikacjaEkspertyza diagnostyczna dotycząca stanu technicznego dwóch linii transmisji mocy (linii wałów) opracowana na podstawie przeprowadzonych pomiarów drgań w 26 punktach pomiarowych, przy jednoczesnej pracy silników napędowych L i PB (wspólnej pracy linii wałów obu burt), w II zakresach ustalonego obciążenia „pół-naprzód” i „cała-naprzód”. Pomiary prędkości i przyspieszeń drgań generowanych przez węzły konstrukcyjne okrętowego układu...
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RAPORT - EKSPERTYZA Z POMIARÓW DRGAŃ LINII WAŁÓW NA JEDNOSTCE ORP „RESKO”
PublikacjaEkspertyza diagnostyczna dotycząca stanu technicznego dwóch linii transmisji mocy (linii wałów) opracowana na podstawie przeprowadzonych pomiarów drgań w 26 punktach pomiarowych, przy jednoczesnej pracy silników napędowych L i PB (wspólnej pracy linii wałów obu burt), w II zakresach ustalonego obciążenia „pół-naprzód” i „cała-naprzód”. Pomiary prędkości i przyspieszeń drgań generowanych przez węzły konstrukcyjne okrętowego układu...
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Comparative study of operation of condensing and traditional boilers equipped with ORC module for electricity generation
PublikacjaThe study analyzed the operation of the "traditional" boiler equipped with the ORC module as the similar arrangement but with the condensing boiler. In the case of a conventional boiler there is noted a greater fuel consumption and the greater power generated than in the case of the unit with the condensing boiler. Postulated is the indicator in the form of a ratio of turbine power to the mass flow rate of fuel, which in turn gives...
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Zwiększenie sprawności procesów technologicznych poprzez zastosowanie układów ORC i systemów trigeneracyjnych
PublikacjaPoprawa sprawności energetycznej procesów technologicznych - obok ograniczenia emisji gazów cieplarnianych i wykorzystania niekonwencjonalnych technologii do konwersji energii - stanowi obecnie najważniejszy element idei zrównoważonego rozwoju. Niniejsza praca wychodzi naprzeciw oczekiwaniom rynkowym, wskazując możliwości wpisania się w ten trend. Stanowi ona zbiór ogólnych wytycznych, opartych o literaturę przedmiotu i własne...
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REPORT Verification expertise of Detroit Diesel engines 16V149TI on the vessel ORP GEN. PUŁASKI
PublikacjaVerification expertise of propulsion engines for generating sets of the ORP GEN. PUŁASKI - type 16V149TI related to a complaint sent by the shipowner to Shiprepair Yard NAUTA S.A.
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RAPORT-EKSPERTYZA Z POMIARÓW DRGAŃ LINII WAŁÓW NA JEDNOSTCE ORP „PIORUN”
PublikacjaEkspertyza diagnostyczna dotycząca stanu technicznego lini transmisji mocy (linii wałów) opracowana na podstawie przeprowadzonych pomiarów drgań. Pomiary prędkości i przyspieszeń drgań generowanych przez węzły konstrukcyjne linii wałów okrętowego układu napędowego wykonano po naprawie głównej napędu okrętu w stoczni „NAUTA”, w celu określenia jego stanu dynamicznego. Rejestrację drgań przeprowadzono w: • płaszczyźnie pionowej (V)...
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Salt melt synthesis of curved nitrogen-doped carbon nanostructures: ORR kinetics boost
PublikacjaImplementing metal-free electrocatalysts for the oxygen reduction reaction (ORR) and revealing crucial chemical or topographical parameters driving their activity are vital for the development of power cells. The carbon-based catalysts are very often synthesized through carbonization of biopolymers, in particular, those one containing nitrogen groups such as chitosan. Unfortunately, the resulting carbonaceous materials usually...
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Comparative study of operation of condensing and traditional boilers equipped with the ORC module for electricity generation
PublikacjaCondensing technology applied to boilers is to make full use of thermal energy contained in the fuel. That means that additionaly the heat from condensation of exhaust gases can be used for the purposes of heating the domestic hot water and to cover the demand for central heating. The study analyzed the operation of the "traditional" boiler equipped with the ORC module as the similar arrangement but with the condensing boiler....
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Waste management in the mining industry of metals ores, coal, oil and natural gas - A review
PublikacjaWaste generated due to mining activity poses a serious issue due to the large amounts generated, even up to 65 billion tons per year, and is often associated with the risk posed by its storage and environmental management. This work aims to review waste management in the mining industry of metals ores, coal, oil and natural gas. It includes an analysis and discussion on the possibilities for reuse of certain types of wastes generated...
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SEM micrographs of aluminium corrosion in alkaline media with various bee products as corrosion inhibitors
Dane BadawczeThis dataset contains various scanning electron microscopy (SEM) micrographs of AA5754 aluminum alloy samples exposed to the corrosive alkaline environment without and with the addition of various bee products to act as green corrosion inhibitors. The products are bee pollen, honey, and putty. They were investigated in bicarbonate buffer (pH =10 or...
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Crystallographic studies of piperazine derivatives of 3-methyl-5-spirofluorenehydantoin in search of structural features of P-gp inhibitors
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Application of specific cell permeable cathepsin G inhibitors resulted in reduced antigen processing in primary dendritic cells
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Does GISSI-AF change the concept of using RAS inhibitors in the primary prevention of atrial fibrillation in hypertensive patients?
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Molecular modelling of transition state analogue inhibitors of glucosamine-6-P synthase and glucose-6-P isomerase.
PublikacjaStruktura kompleksu 2-amino-2-deoksy-D-glucitolo-6-P (ADGP) z centrum aktywnym syntazy GlcN-6-P z E. coli została wykorzystAna jako punkt wyjścia do modelowania molekularnego analogów ADGP. Używając programu GROMOS96 wygenerowano konformacje analogów o najniższych energiach wewnętrznych, które następnie ''dokowano'' w centrum aktywnym enzymu. Dokonano syntezy wybranych związków i określono parametry kinetyczne i termodynamiczne...
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Correction to “Emerging Anticancer Activity of Candidal Glucosamine-6-Phosphate Synthase Inhibitors upon Nanoparticle-Mediated Delivery”
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Structural and Evolutionary Analysis Indicate that the SARS-CoV-2 Mpro is an Inconvenient Target for Small-Molecule Inhibitors Design
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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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Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates
PublikacjaIn the present work, we described convenient methods for the synthesis ofN-thiophosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates as steroid sulfatase(STS) inhibitors. To design the structures of the potential STS inhibitors, molecularmodeling techniques were used. A computational docking method was used to deter-mine the binding modes of the synthesized inhibitors as well as to identify potentialinteractions between specified...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublikacjaThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors
PublikacjaAlzheimer’s disease (AD), also called senile dementia is a neurodegenerative disease seen commonly in the elderly and is characterised by the formation of β-amyloid plaques and neurofbrillary tangles (NFT). Though a complete understanding of the disease is lacking, recent studies showed the role of the enzyme acetylcholinesterase (AChE) in pathogenesis. Finding new lead compounds from natural sources has always been a quest for...
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Spectroscopic properties of high-temperature sintered SrS:0.05%Ce3+ under high hydrostatic pressure
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Wstępna koncepcja doboru czynnika roboczego obiegu ORC dla określonych źródeł ciepła odpadowego
PublikacjaW procesach technologicznych ciepło odpadowe stanowi nie zawsze do końca rozwiązany problem. Zagospodarowanie tego ciepła, szczególnie w przemyśle rafineryjnym i petrochemicznym, napotyka na wiele problemów, związanych z niską egzergią, znacznym rozproszeniem, dużym zróżnicowaniem parametrów i opłacalnością potencjalnej modernizacji. Jedną z obiecujących tutaj technologii utylizacji tego ciepła jest zastosowanie układu ORC. Przeprowadzono...
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ORF Approximation in Numerical Analysis of Fractional Point Kinetics and Heat Exchange Model of Nuclear Reactor
PublikacjaThis paper presents results concerning numerical solutions of the fractional point kinetics (FPK) and heat exchange (HE) model for a nuclear reactor. The model consists of a nonlinear system of fractional and ordinary differential equations. Two methods to solve the model are compared. The first one applies Oustaloup Recursive Filter (ORF) and the second one applies Refined Oustaloup Recursive Filter (RORF). Simulation tests have...
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ORF Approximation in Numerical Analysis of Fractional Point Kinetics and Heat Exchange Model of Nuclear Reactor
PublikacjaThis paper presents results concerning numerical solutions of the fractional point kinetics (FPK) and heat exchange (HE) model for a nuclear reactor. The model consists of a nonlinear system of fractional and ordinary differential equations. Two methods to solve the model are compared. The first one applies Oustaloup Recursive Filter (ORF) and the second one applies Refined Oustaloup Recursive Filter (RORF). Simulation tests have...
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Utilisation of bleed steam heat to increase the upper heat source temperature in low-temperature ORC
PublikacjaW pracy przedstawiono możliwość dogrzewu obiegu ORC za pomocą pary upustowej.
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Analiza możliwości odzyskiwania ciepła odpadowego w przemyśle rafineryjnym z wykorzystaniem układów ORC
PublikacjaJednym z najważniejszych zagadnień współczesnej techniki jest poszukiwanie nowych możliwości pozyskiwania energii elektrycznej poprzez zagospodarowanie dotychczas niewykorzystanych lub bezużytecznie marnowanych jej źródeł. Jest to niezwykle ważna kwestia zarówno z ekonomicznego, technologicznego, jak i środowiskowego punktu widzenia. Jednym z przykładów nowoczesnych rozwiązań w tej dziedzinie może być zastosowanie układu opartego...
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Systematic and Selection Criteria for ORC System Working Fluid Used for a Determined Amount of Excessive Energy
PublikacjaPoprawa sprawności energetycznej procesów technologicznych stanowi obecnie - obok ograniczenia emisji gazów cieplarnianych i wykorzystania alternatywnych źródeł do produkcji energii - najważniejszy element idei zrównoważonego rozwoju. Niniejsza praca wychodzi naprzeciw rynkowym oczekiwaniom. wskazując możliwości wpisania się w ten trend. W procesach technologicznych ciepło odpadowe stanowi nie zawsze do końca rozwiązany problem....
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Wpływ wariantów termodynamicznych układów ORC i systemów trigeneracyjnych na poprawę ich sprawności
PublikacjaNiniejsza praca przedstawia systemowe podejście do problemu uzyskania optymalnej sprawności układów ORC (Organic Ranking Cycle), przy uwzględnieniu jako kryterium zarówno sprawności termodynamicznej, ekologicznego wpływu czynnika termodynamicznego na środowisko oraz kryteriów doboru rodzaju czynnika z punktu widzenia jego oceny i temperaturowych warunków pracy.