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Search results for: MEDICINAL BENEFITS
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Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds
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Design, synthesis and in vitro biological evaluation of a small cyclic peptide as inhibitor of vascular endothelial growth factor binding to neuropilin-1
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Branched pentapeptides as potent inhibitors of the vascular endothelial growth factor 165 binding to Neuropilin-1: Design, synthesis and biological activity
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Low-Barrier Hydrogen Bond Determines Target-Binding Affinity and Specificity of the Antitubercular Drug Bedaquiline
PublicationThe role of short strong hydrogen bonds (SSHB) in ligand-target binding remains largely unexplored, thereby hin- dering a potentially important avenue in the rational drug de- sign. Here, we investigate the interaction between bedaquiline (Bq), a potent anti-tuberculosis drug, and the mycobacterial ATP synthase, to unravel the role of a specific hydrogen bond to a conserved acidic residue in the target affinity and specificity....
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublicationFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry
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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublicationConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublicationA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents
PublicationA series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic...
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublicationThe 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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Study of the anticancer potential of Cd complexes of selenazoyl-hydrazones and their sulfur isosters
PublicationThe biological activity of Cd compounds has been investigated scarce since Cd has been recognized as a human carcinogen. However, the toxicity of cadmium is comparable to the toxicity of noble metals such as Pt and Pd. The paradigm of metal toxicity has been challenged suggesting that metal toxicity is not a constant property, yet it depends on many factors like the presence of appropriate ligands. Studies on anticancer activity...
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublicationMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublicationNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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Synthesis and biological activity of novel ester derivatives of N3-(4-metoxyfumaroyl)-(S)-2,3-diaminopropanoic acid containing amide and keto function as inhibitors of glucosamine-6-phosphate synthase
PublicationA short series of novel ester derivatives of N3-4-methoxyfumaroyl-(S)-2,3-diaminopropanoic acid (FMDP) containing amido or keto functions have been designed and synthesized. Their antifungal activity and inhibitory properties toward fungal glucosamine-6-phosphate synthase has also been evaluated. The obtained compounds 11-13 and 15-17 demonstrated good antifunga activity against Candida albicans. Compounds 11-13 displayed also...
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublicationMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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The parallel environment for endoscopic image analysis
PublicationThe jPVM-oriented environment to support high performance computing required for the Endoscopy Recommender System (ERS) is defined. SPMD model of image matching is considered and its two implementations are proposed: Lexicographical Searching Algorithm (LSA) and Gradient Serching Algorithm (GSA). Three classes of experiments are considered and the relative degree of similarity and execution time of each algorithm are analysed....
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Heat transfer characteristics of hybrid microjet -microchannel cooling module
PublicationThe paper presents the experimental investigation of heat transfer intensification in a microjet- microchannel cooling module. Applied technology takes benefits from two very attractive heat removal techniques. When jets are impinging on the surface, they have a very high kinetic energy at the stagnation point, also in microchannels boundary layer is very thin allowing to obtain very high heat fluxes. Main objective of this paper...
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The Impact of urban Localizations on the Growth Possibilities for Small Firms
PublicationThe purpose of this study was to identify the differences in the profiles of firms and their owners in urban and non-urban locations and also to asses the impact of those differences on the possibilities of growth for firms from both types of locations. Findings: urban entrepreneurs are better educated, more experienced and more positively motivated. Their firms are more innovative, with more qualified employeesadn better access...
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In search of the new: American volunteers’ opinions about their participation in the Teaching English in Poland (TEIP) Program
PublicationThe Teaching English in Poland (TEIP) program relies on summer camps during which native English speakers, American volunteers, teach Polish children and adolescents using the language immersion method – during everyday activities, sports and art classes, and similar occasions. A vital aspect of the evaluation of the program is researching its impact on the young people; however, the opinions of the volunteers regarding their...
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Magnetic superhydrophobic melamine sponges for crude oil removal from water
PublicationThis paper proposes the preparation of a new sorbent material based on melamine sponges (MS) with superhydrophobic, superoleophilic, and magnetic properties. This study involved impregnating the surface of commercially available MS with eco-friendly deep eutectic solvents (DES) and Fe3O4 nanoparticles. The DES selection was based on the screening of 105 eutectic mixtures using COSMO-RS modeling. Other parameters affecting the efficiency...
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The Impact of Hybrid Flame Retardant Compositions on the Performance of Foamed Flexible Polyurethane/Ground Tire Rubber Composites
PublicationCurrent sustainability-oriented trends affect polyurethane (PU) materials and stimulate the incorporation of recycled or waste-based materials as fillers. Ground tire rubber (GTR) poses as an auspicious candidate due to the excellent performance of car tires. Despite the benefits related to the mechanical performance, it contributes to the increasing flammability of the resulting composites. Herein, presented work assessed the...
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Slowly-closing valve behaviour during steam machine accelerated start-up
PublicationThe paper discusses the state of stress in a slowly-closing valve during accelerated start-up of a steam turbine. The valve is one of the first components affected by high temperature gradients and is a key element on which the power, efficiency and safety of the steam system depend. The authors calibrated the valve model based on experimental data and then performed extended Thermal-FSI analyses relative to experiment. The issue...
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Membrane distillation assisting food production processes of thermally sensitive food liquid items: a review
PublicationPhysical separation technologies have become important tool for processing in the current food manufacturing industries, especially for the products containing bioactive compounds thanks to their health benefits in costumers. As for the processing of bioactive food ingredients implies the implementation of integrated systems oriented to their separation, fractionation, and recovery. In this field, membrane distillation (MD), which...
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Mangiferin: A comprehensive review on its extraction, purification and uses in food systems
PublicationWith the target of fabricating healthier products, food manufacturing companies look for natural-based nutraceuticals that can potentially improve the physicochemical properties of food systems while being nutritive to the consumer and providing additional health benefits (biological activities). In this regard, Mangiferin joins all these requirements as a potential nutraceutical, which is typically contained in Mangifera indica...
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How digital platforms support public values through government-citizen collaboration?
PublicationDigital platforms are becoming a popular means of multi-sided interactions between public institutions and their constituents. By enabling information sharing, consultation, and other forms of government-citizen collaboration, they facilitate co-decision-making and co-creation. Although digital platforms are not, the mechanism through which they can create public value, although important for government institutions and citizens...
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Young shoots of red cabbage are a better source of selected nutrients and glucosinolates in comparison to the vegetable at full maturity
PublicationCruciferous vegetables are a valuable source of ingredients with health benefits. The most characteristic compounds of cruciferous vegetables with identified anticancer properties are glucosinolates. Young shoots and sprouts of red cabbage are becoming a popular fresh food rich in nutrients and bioactive compounds. The objective of this research was to determine, for the first time in a comprehensive approach, whether young shoots...
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A Wideband Rotary-Joint-Free H-Plane Horn Antenna With 360° Steerable Radiation Pattern Using Gap Waveguide Technology
PublicationConsidering the limitations of electronically steerable antennas such as limited steering span, gain degradation for large steering angles, complexity, and cost, this article is focused on the design of a simple mechanically steerable H-plane horn antenna. It is shown that since there is no need for an electrical connection between the top and bottom sections of a gap waveguide (GWG), if a sectoral horn is properly designed and realized...
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Social Media and Knowledge Sharing – What Do We Know So Far?
PublicationThe aim of this paper is to examine previous studies on topic of social media and how it influences knowledge sharing online and thereafter establish respective body of knowledge. The background investigation has been organized as a theoretical review with qualitative premises. The multi-layered Systematic Literature Review process has been utilized and carried out to fetch the most relevant peer-reviewed researches in the past....
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Increasing the Seismic Resistance of Wood-frame Buildings by Applying PU Foam as Thermal Insulation
PublicationWood-frame buildings are very common in regions that are exposed to earthquakes. Most of residential buildings are constructed using this technology; therefore, the seismic resistance of them is really essential in order to prevent human losses and structural damage. The aim of the present article is to show the results of the detailed numerical FEM analysis focused on the seismic behaviour of the wood-frame house with different...
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Heat recovery from the hybrid photovoltaic tile – experimental studies with the solar light simulator
PublicationConsidering the current development of micro-cogeneration energy sources, supported by the national prosumer policy and the act on the renewable energy sources, there is a great demand for the effective solar technologies. In this area, the photovoltaic cells with a combined conversion of the solar radiation energy into the electrical and thermal energy (PV/T cells) seem to be attractive. They are already widely available and treated...
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The usefulness of birch saps from the area of Podkarpacie to produce birch syrup
PublicationIn northern European countries, as well as in North America tree saps of maples and birches are used for the production of syrups. Birch syrups are characterized by a specific aromatic taste and can be used as an addition to sweets, desserts, salads and meats. Attention is paid to the health benefits of birch syrups, mainly for high mineral content. The aim of this study was to evaluate the usefulness of birch saps obtained from...
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Imunofan—RDKVYR Peptide—Stimulates Skin Cell Proliferation and Promotes Tissue Repair
PublicationRegeneration and wound healing are vital to tissue homeostasis and organism survival. One of the biggest challenges of today’s science and medicine is finding methods and factors to stimulate these processes in the human body. Effective solutions to promote regenerative responses will accelerate advances in tissue engineering, regenerative medicine, transplantology, and a number of other clinical specialties. In this study, we...
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Attitudes of oncology patients’ towards biospecimen donation for biobank research
PublicationBackground Since the biological material that remains after diagnostic and therapeutic procedures plays crucial role in biobank research, this study aims to explore cancer patients’ views on the donation of biospecimens for research purposes. Methods 548 oncology patients from two hospitals with oncology treatment units in Poznan, Poland,...
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Specialist Pavilion Hospitals Of West Prussia In The 19th Century – Evolution Of The Idea
PublicationThe size and shape of the largest pavilion hospitals established in West Prussia in the 19th century changed along with the advancing technical and medical knowledge, the progress of ideas regarding modern society, architectural patterns, and the needs for which the hospitals were built. Apart from the medical treatment section, there were administrative, social and technical facilities, all constituting parts of the complex. The...
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Assessment of hearing in coma patients employing auditory brainstem response, electroencephalography, and eye-gaze-tracking
PublicationThe results of the study conducted by Tagliaferri et al. in 12 European countries indicate that the ratio of registered brain injury cases in Europe amounts to 150-300 per 100 000 people, with the European mean value of 235 cases per 100 000 people. The project presented in the paper assumes development of a combined metric of patients’ state remaining in coma by intelligent fusion of GCS (subjective Glasgow Coma Scale or its derivatives)...
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Market Structure and Market Power in Selected Sectors of The Polish Economy Based on COICOP Classification
PublicationThis paper present new and simple measures of market structure and market power. Based on the classical models of market structures, where a given structure is determined by the number of enterprises, indexes of degree of monopoly have been estimated, representing an average number of entities per branch. Additionally, market power indexes have been determined as an average revenue per an enterprise in a given branch. This approach...
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Instrumental techniques used in the analysis of exhaled air
PublicationExhaled air composition changes depending on the health status of the patient, making it possible to use breath analysis for diagnosis and monitoring purposes. Despite the fact that it is not yet used in every day medical practice, it potential application could facilitate the diagnostics of various diseases such as metabolic disorders, respiratory tract and gastrointestinal diseases. Described in this paper are different application...
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Meeting Requirements Imposed by Secure Software Development Standards and Still Remaining Agile
PublicationThe paper introduces the AgileSafe method of selecting agile practices for software development projects that are constrained by assurance requirements resulting from safety and/or security related standards. Such requirements are represented by argumentation templates which explain how the evidence collected during agile practices implementation will support the conformity with the requirements. Application of the method is demonstrated...
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Digital Photogrammetry in the Analysis of the Ventricles' Shape and Size
PublicationThis article presents spatial analyzes conducted to assess the potential of ReMake software to be used for medical purposes, with emphasis on the analysis of the shape and dimensions of the ventricles. To achieve this goal, the length of the sections measured with the ReMake and Image Master programs have been compared. RMS error was on the level of 1.2 mm. In addition to indicating the appropriateness of using this software, there...
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The influence of rest interval on total training load during 10 sets of the bench press exercise performed to concentric failure
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Bezzałogowe środki latające (BSL) w układzie czterowirnikowego helikoptera
PublicationRozwój układów sterowania, kamer pracujących w świetle widzialnym oraz w podczerwieni doprowadził do wzrostu znaczenia bezpilotowych środków latających. Bezpilotowe środki latające wykorzystywane są do realizacji celów zarówno wojskowych, jak i cywilnych. Podstawowymi zaletami bezpilotowych środków latających są: małe wymiary, duża mobilność, niskie koszty wytworzenia i eksploatacji. Użytkowanie bezpilotowych środków latających...
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Analiza sentymentu jako narzędzie monitorowania wyników finansowych przedsiębiorstwa
PublicationMedia społecznościowe tworzą globalną platformę do dzielenia się interesującymi pomysłami lub nowościami, komentarzami i recenzjami. Stanowią bogate źródło danych do eksploracji opinii w celu pozyskania wcześniej nieznanej i użytecznej wiedzy biznesowej, która umożliwi nie tylko zwinne zarządzanie na rzecz skutecznej obsługi klienta, ale również powinna mieć odzwierciedlenie w finansowych wynikach przedsiębiorstwa. Za główny cel...
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Methodological issues of functional safety and reliability assessment of critical systems in industrial hazardous plants
PublicationThe aim of this article is to identify and discuss some methodological issues that are of interest among functional safety specialists and experts after publication of the second edition of international standards IEC 61508 and IEC 61511, including the design and implementing the safety-related functions of higher safety integrity levels and protection layers. The basic role of safety-related systems is to reduce effectively and...
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Centrifugal magnetic fluid seals
PublicationSeals perform an important and at times overlooked function in a lubricant system. They prevent or minimize the movement of the lubricant between two surfaces and also minimize the level of contamination in the system. Seals are divided into static and dynamic types. Static seals operate in systems where the mating surfaces do not move relative to each other. In contrast, dynamic seals operate under conditions where the mating surfaces...
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Optimized Space Vector Modulation strategy for five phase voltage source inverter with third harmonic injection
PublicationThis paper presents a simple and an effective SVM algorithm for five-phase Voltage-Source Inverters with the possibility to control independently the voltage vectors for fundamental and auxiliary orthogonal subspaces. The essential benefit is that output voltage is generated using only four active voltage vectors with limited numbers of switching. In the proposed solution, four active vectors are arbitrary chosen, independent of...
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A competition between two- and three-body dissociation channels in photo-double-ionization of tetrahydro-2H-pyran and 3,4-dihydro-2H-pyran molecules
PublicationVarious molecules possess structures consisting of the heterocyclic rings containing oxygen atoms. These substances often play a significant role in many different fields of chemistry, medicine, and biology. Due to a specific atomic composition and bond arrangement, many of these molecules retain unique electronic properties, which may be probed by diverse spectroscopic techniques, including those utilizing synchrotron radiation....
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Praca bibliotekarza w erze cyfrowej: 20 darmowych programów i aplikacji do wykorzystania w bibliotece
PublicationArtykuł prezentuje 20 darmowych programów komputerowych, wykorzystywanych w Bibliotece Głównej Gdańskiego Uniwersytetu Medycznego. Przedstawione aplikacje mogą wzbogacić warsztat pracy bibliotekarzy, którzy zajmują się: tworzeniem szkoleń, edycją bibliotecznych stron internetowych oraz komunikacją z użytkownikami.
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Stabilization of N-, N,N-, N,N'-Methylated and Unsubstituted Simple Amidine Salts by Multifurcated Hydrogen Bonds
PublicationIn the light of the usefulness of amidines in medicinal chem., this paper considers the effects on biol. properties and chem. reactivities of org. mols. affected by intramol. interactions. The study of chem. shifts has been an important source of information on the electronic structure of amidine salts and their ability to form non-covalent bonds with nucleic acids. The NMR and IR results demonstrate that hydrogen bonds are...
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Description logic based generator of data-centric applications
PublicationThe knowledge stored in Ontology Management Systems (OMS) that originally has the form of expressions, can be seen as a user application specification or as knowledge provided by an expert. The generator of applications discussed in this paper is defined as a program that automatically generates an application that meets a certain specification stored in OMS. It is shown that it is possible to build a user interface for data management...
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Description logic based generator of data-centric applications
PublicationThe knowledge stored in Ontology Management Systems (OMS) that originally has the form of expressions, can be seen as a user application specification or as knowledge provided by an expert. The generator of applications discussed in this paper is defined as a program that automatically generates an application that meets a certain specification stored in OMS. It is shown that it is possible to build a user interface for data management...