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Wyniki wyszukiwania dla: AGENT
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Contribution of UDP-glucuronosyltransferases (UGTs) in metabolism of acridinone antitumor agents, C-1311, C-1305, and their less active structural analogues, C-1330 and C-1299
PublikacjaCelem prowadzonych badań było określenie roli UDP-glukuronylotransferaz, uważanych za najważniejsze enzymy detoksykujące, w metabolizmie pochodnych imidazo- i triazoloakrydonu. Wykazano, że najbardziej aktywne przeciwnowotworowo związki z obu grup, tj. C-1311 i C-1305 są transformowane do O-glukuronidów, w przeciwieństwie do ich metoksylowych analogów, odpowiednio związku C-1330 i C-1299. Analiza składu mieszanin reakcyjnych zawierających...
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Antibiotic resistance in Staphylococcus aureus strains isolated from cows with mastitis in the eastern Poland and analysis of susceptibility of resistant strains to alternative non-antibiotic agents: lysostaphin, nisin and polymyxin B.
PublikacjaThe aim of the studies was analysis of resistance of Staphylococcus aureus isolates from bovine mastitis in eastern part of Poland to a set of 20 antibiotics and three alternative agents: lysostaphin, nisin and polymyxin B. Eighty-six out of 123 examined isolates were susceptible to all of 20 tested antibiotics (70 %). The highest percentage of resistance was observed in the case of β-lactam antibiotics: amoxicillin (n=22, 17.9...
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublikacjaInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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2,7-Dihydro-3H-pyridazino[5,4,3-kl]acridin-3-one derivatives, novel type of cytotoxic agents active on multidrug-resistant cell lines. Synthesis and biological evaluation.
PublikacjaOtrzymano serię pirydazyno akrydyn-3-onów w reakcji 9-okso-9,10-dihydroakrydyno-1-karboksylanu etylu z POCl3, następnie dodanie odpowiedniej alkiloaminoalkilohydrazyny. Badane związki wykazują w porównaniu z referencyjnymi cytostatykami DX, MIT niższe wartości indeksu RI, a także niższe aktywności cytotoksyczne.
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Human CYP2 family of cytochrome P-450 takes part in metabolism of two acridine antitumor agents, C-1311 and C-1748, selected for I phase of clinical trials
PublikacjaPraca zawiera wyniki badań metabolicznej transformacji przeciwnowotworowych pochodnych akrydyny wobec zestawu 16 prób enzymów mikrosomalnych, pochodzących z wątroby 16 różnych pacjentów. Wykazano, że za metabolizm tych związków u człowieka odpowiedzialne są głównie izoenzymy z rodziny CYP2.
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Synthesis and biological evaluation of 2,7-Dihydro-3H-dibenzo[de,h]cinnoli- ne-3,7-done derivatives a novel group of anticancer agents active on a multidrug resistance cell line.
PublikacjaZsyntezowano serię pochodnych pirydazonu z jednym lub dwoma łańcuchami bocznymi w różnych pozycjach chromoforu tetracyklicznego. Związki wykazały aktywność cytoksyczną na mysią białaczkę L1210 i ludzką k562 oraz na linii komórkowej oporności krzyżowej MDR (k562/DX). Dwa najbardziej aktywne związki przetestowano in vivo na mysiej białaczce P388. Wykazały one aktywność przeciwnowotworową porównywalną z aktywnością Mitoxantronu.
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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
PublikacjaA 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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Phytotoxic Metabolites from Three Neofusicoccum Species Causal Agents of Botryosphaeria Dieback in Australia, Luteopyroxin, Neoanthraquinone, and Luteoxepinone, a Disubstituted Furo-α-pyrone, a Hexasubstituted Anthraquinone, and a Trisubstituted Oxepi-2-one from Neofusicoccum luteum
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Method-Dependent Epidemiological Cutoff Values for Detection of Triazole Resistance in Candida and Aspergillus Species for the Sensititre YeastOne Colorimetric Broth and Etest Agar Diffusion Methods
PublikacjaAlthough the Sensititre Yeast-One (SYO) and Etest methods are widely utilized, interpretive criteria are not available for triazole susceptibility testing of Candida or Aspergillus species. We collected fluconazole, itraconazole, posaconazole, and voriconazole SYO and Etest MICs from 39 laboratories representing all continents for (method/agent-dependent) 11,171 Candida albicans, 215 C. dubliniensis, 4,418 C. glabrata species complex,...
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Complete Nucleotide Sequence of the pCTX-M3 Plasmid and Its Involvement in Spread of the Extended-Spectrum β-Lactamase GeneblaCTX-M-3
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Mosaic Structure of p1658/97, a 125-Kilobase Plasmid Harboring an Active Amplicon with the Extended-Spectrum β-Lactamase Gene bla SHV-5
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Nonstationary Pharmacokinetics of Caspofungin in ICU Patients
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Phenethyl Isothiocyanate Inhibits Shiga Toxin Production in Enterohemorrhagic Escherichia coli by Stringent Response Induction
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Enhanced susceptibility to antifungal oligopeptides in yeast strains overexpressing ABC multidrug efflux pumps
PublikacjaPorównano podatność na działanie związków przeciwgrzybowych o strukturze oligopeptydowej oraz aminokwasowej szczepów Saccharomyces cerevisiae z usuniętymi genami kodującymi białka oporności wielolekowej oraz transformantów tych szczepów, zawierających geny CDR1, CDR2 lub MDR1, kodujące główne pompy wielolekowe Candida albicans. Rekombinowane szczepy nadprodukujące białka Cdr1p i Cdr2p wykazywały zwiększoną wrażliwość na wszystkie...
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Molecular typing of clinical isolates of Escherichia coli by a new PCR MP method
PublikacjaTypowanie epidemiologiczne bakterii jest rutynową procedurą stosowaną w badaniach zakażeń szpitalnych i wymaga stosowania odpowiednich metod o wysokim potencjale różnicującym. Przedstawiliśmy możliwości nowej techniki PCR MP w różnicowaniu szczepów E. coli. Rezultaty zostały porównane z wynikami uzyskanymi metodą PFGE.
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The gaseous messenger carbon monoxide is released from the eye into the ophthalmic venous blood depending on the intensity of sunlight
PublikacjaCircadian and seasonal rhythms in daylight affect many physiological processes. In the eye, energy of intense visible light not only initiates a well-studied neural reaction in the retina that modulates the secretory function of the hypothalamus and pineal gland, but also activates the heme oxygenase (HO) to produce carbon monoxide (CO). This study was designed to determine whether the concentration of carbon monoxide (CO) in the...
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Cytochromes P450 and Skin Cancer: Role of Local Endocrine Pathways
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Synthesis of Combretastatin A-4 Analogs and their Biological Activities
PublikacjaCombretastatin A-4 (CA-4) is a natural product, which consists of two phenyl rings, linked by an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Mrówczan sodu z nowym pakietem inhibitorów korozji jako ekologiczny środek do odladzania infrastruktury lotniczej.
PublikacjaPrzedstawiono wyniki badań korozji kadmowej powłoki na stali oraz korozji po zanurzeniu stopów metali w mrówczanie sodu z nowym pakietem inhibitorów korozji, zawierającym synergiczną kompozycję poliasparaginianu sodu oraz imidazolu. Ponadto wyznaczono zdolność penetracji lodu przez badany układ. Właściwo- ści opracowanej kompozycji odladzającej porównano z właściwościami środków dostępnych na rynku. Uzyskane wyniki wskazują, że otrzymany...
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Consolidating logs in varying formats into a structured repository = konsolidacja logów w zmiennych formatach do strukturalnego repozytorium
PublikacjaDuring 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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Reliable Document-Centric Processing in Loosely Coupled Email-Based Systems
PublikacjaEmail is a simple way to exchange digital documents of any kind. The Mobile INteractive Document architecture (MIND) enables self-coordination and self-steering of document agent systems based on commonly available email services. In this paper, a mechanism for providing integrity and reliability of such an email based agent system is proposed to cope with message soft or hard bounces, user interrupts, and other unexpected events....
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Collision-free network exploration
PublikacjaMobile agents start at different nodes of an n-node network. The agents synchronously move along the network edges in a collision-free way, i.e., in no round two agents may occupy the same node. An agent has no knowledge of the number and initial positions of other agents. We are looking for the shortest time required to reach a configuration in which each agent has visited all nodes and returned to its starting location. In...
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A New Approach to Chemical Recycling of Polyamide 6.6 and Synthesis of Polyurethanes with Recovered Intermediates
PublikacjaA new efficient method for the chemical decomposition of polyamide 6.6 by the glycolysis and amino-glycolysis processes was proposed. The glycolysis was conducted using the mass excess of ethylene glycol (EG) as a decomposing agent in the presence of a catalyst. Also, a mixture of EG and triethylenetetramine was used as another decomposing agent in the amino- glycolysis process. The described process of decomposition did not...
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Properties of chitosan/CuNPs coatings electrophoretically deposited on TiO2 nanotubular oxide layer of Ti13Zr13Nb alloy
PublikacjaCoatings based on chitosan/CuNPs (chit/CuNPs) were obtained by a one-step electrophoretic deposition (EPD) on nanotubular oxide layer of Ti13Zr13Nb alloy. The deposition was carried out for 1 min applying voltages of 10 and 20 V with and without the addition of dispersing agent (Polysorbate 20) to the suspension. The coatings obtained for the lower voltage were more uniform than for the higher voltage. By adding a dispersing agent,...
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Integrated monitoring, control and security of Critical Infrastructure Systems
PublikacjaModern societies have reached a point where everyday life relies heavily on desired operation of critical infrastructures, in spite of accidental failures and/or deliberate attacks. The issue of desired performance operation of CIS at high security level receives considerable attention worldwide. The pioneering generic methodologies and methods are presented in the paper project for designing systems capable of achieving these...
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Collision-Free Network Exploration
PublikacjaA set of mobile agents is placed at different nodes of a n-node network. The agents synchronously move along the network edges in a collision-free way, i.e., in no round may two agents occupy the same node. In each round, an agent may choose to stay at its currently occupied node or to move to one of its neighbors. An agent has no knowledge of the number and initial positions of other agents. We are looking for the shortest possible...
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Integration of brood units in game universe
PublikacjaAn access to a great number of various services allows for decomposition of complex problems Developing a game universe usually involves creation of various units which can be encountered by a player. Those can be lonely or organized in broods animals and monsters wandering around the game world. In order to provide natural gaming experience those units should behave variously depending on the world situation. Those behaviours...
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Model of management of knowledge bases in the information technology evaluation environment
PublikacjaThe 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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Old Problems - New Solutions: Conversion of Capitals as a Tool for Shaping the Competitive Position in the Economic Field
PublikacjaThe acts and operations any social actor effectuates in each of the logically distinguished spheres of reality are conditioned by many factors, among which a reliable analysis of the strengths and weaknesses of an agent should be considered of utmost importance. The concept of capitals presented in this article divides the quantity of resources available to all acting agents into four main categories (which allows for determining...
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Old Problems - New Solutions: Conversion of Capitals as a Tool for Shaping the Competitive Position in the Economic Field
PublikacjaThe acts and operations any social actor effectuates in each of the logically distinguished spheres of reality are conditioned by many factors, among which a reliable analysis of the strengths and weaknesses of an agent should be considered of utmost importance. The concept of capitals presented in this article divides the quantity of resources available to all acting agents into four main categories (which allows for determining...
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Examination of the epoxy coating system's resistance to Corrobill
PublikacjaThe tests of the influence of the surface cleaning agent on the epoxy coating were carried out. Electrochemical and corrosion tests were carried out. The effect of the preparation on the adhesion and hardness of the tested coating was tested.
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Drawing maps with advice
PublikacjaRozważamy następujący problem obliczeniowy. Agent zostaje umieszczony w wierzchołku nieznanego mu grafu. Wierzchołki grafu są nierozróżnialne, natomiast krawędzie posiadają numery portów. Zadaniem agenta jest wyznaczenie mapy, tzn. obliczenie izomorficznej kopii grafu, lub obliczenie dowolnego drzewa spinającego grafu. Bez dodatkowej informacji zadań tych nie można wykonać. W artykule wyznaczamy oszacowania na minimalną liczbę...
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Knowledge management in the processes of project requirements analysis
PublikacjaAuthors, based on one of popular software project management methods as RUP fo-cused on one of most important discipline in project management as requirements management. Authors decomposed the role of the business analyst and present methodological and realizational processes of knowledge managament in traditional and applied sources of knowledge tied with this role. An experiment was conducted in four project teams of all sizes,...
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The impact of the temperament model on the behavior of an autonomous driver
PublikacjaBecause it is generally believed that the personality and temperament of a human driver influence his/her behavior on the road, the article presents a computational model of the temperament of an autonomous agent - a driver. First, a short review of the four ideas of Galen’s temperament in psychology is presented. Temperament traits are grouped into four other sets, one of which is chosen for implementation in the project of integration...
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Kinetics of the crosslinking reaction between genipin and chitosan solutions
PublikacjaThe kinetics of the chitosan crosslinking reaction with genipin was examined. The strong relationship was found between crosslinking agent concentration, chitosan concentration, temperature and gelling time. Data obtained will be used in the proper selection of optimal genipin concentration for crosslinking chitosan solutions.
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The dying medium temperature impact on the final moisture content of pine wood at constant drying time
PublikacjaThe results of final moisture content of pine wood (Pinus sylvestris L.) after drying process are presented. The wood in the experiments was taken from the northern part of Pomeranian region in Poland. The drying process was performed in the experimental chamber equipped with the micro-jet heat exchanger. The air at temperatures of 40°C, 60°C, 80°C, 100°C and 120°C with relative humidity about 60% and atmospheric pressure was the...
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Ultrasound-assisted deep eutectic solvent-based liquid–liquid microextraction for simultaneous determination of Ni (II) and Zn (II) in food samples
PublikacjaA new approach was developed for the simultaneous pre-concentration and determination of Ni (II) and Zn (II) in food samples. This method is based on ultrasound-assisted liquid–liquid micro extraction using hydrophobic deep eutectic solvent (DES) and 1,10-phenanthroline as chelating agent. The effect of several parameters, such as pH, selection and volume of DES, amount of chelating agent, time of sonication and centrifugation,...
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Recycling of Polyurethanes
PublikacjaPolyurethane waste can be recycled by mechanical methods (i.e., grinding and applying as a filler or pressing with a bonding agent) and chemical methods (mainly by e.g., glycolysis, hydrolysis, or aminolysis). There is also possibility to the recover energy from polyurethanes waste (by incineration, gasification, and pyrolysis).
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Modelowanie i ograniczanie skutków ataków uzurpacji uprawnień w systemach teleinformatycznych wspierających różnicowanie poziomu QoS
PublikacjaW wieloagentowych systemach teleinformatycznych pracujących w paradygmacie Klient-Serwer i wspierających różnicowanie poziomu QoS poważnym zagrożeniem są ataki uzurpacji uprawnień metodą Fałszywego VIPa. Ich celem jest zapewnienie Klientowi nienależnie wysokiego poziomu QoS, co powoduje nadużycie zasobów Serwera i szkody dla innych Klientów. W referacie podjęto próbę sforma-lizowania modelu takich ataków oraz zaproponowa-no obustronnie...
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Convenient and efficient N-methylation of secondary amines under solvent-free ball milling conditions
PublikacjaIn the present work, we report the development of a rapid, efcient, and solvent-free procedure for the N-methylation of secondary amines under mechanochemical conditions. After optimization of the milling parameters, a vibrational ball mill was used to synthesize 26 tertiary N-methylated amine derivatives in a short time of 20 min (30 Hz frequency) and high yields ranging from 78 to 95%. An exception was compounds having a hydroxyl...
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Security Information Sharing for the Polish Power System
PublikacjaThe Polish Power System is becoming increasingly more dependent on Information and Communication Technologies which results in its exposure to cyberattacks, including the evolved and highly sophisticated threats such as Advanced Persistent Threats or Distributed Denial of Service attacks. The most exposed components are SCADA systems in substations and Distributed Control Systems in power plants. When addressing this situation...
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Atom-economic thiophosphoroselenenylations of C–H acid esters and amides
PublikacjaThree improved thiophosphoroselenenylation procedures of CHacids, including derivatives of malonic and acetyl-, phosphono-, 4-nitrophenyl- and 3-pyridylacetic acids, have been described and compared to previously reported thiophosphoroselenylation of diethyl malonate using bis(disopropoxyphosphinothioyl)diselenide alone or with the aid of methyl iodide. The use of iodine makes it possible to utilize both equivalents of the selenenylating...
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Reputacja i zaufanie w systemach teleinformatycznych z podmiotami anonimowymi podejście dynamiczne
PublikacjaAbstrakcją współczesnego systemu teleinformatycznego jest system wieloagentowy z autonomicznymi, racjonalnymi i wirtualnie anonimowymi agentami wchodzącymi we wzajemne interakcje dla wymiany usług. W referacie uzasadniono konieczność projektowania dla niego podsystemu budowy reputacji i zaufania oraz odpowiednich analiz w ujęciu dynamicznym. Dokonano przeglądu motywacyjnie zgodnych mechanizmów uczciwego raportowania usług oraz...
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Protokół głosowania większościowego w narzędziu wsparcia decyzji handlowych
PublikacjaIstnieje szerokie spektrum narzędzi i metod wspierających decyzje handlowe, lecz brakuj jasnych reguł ich stosowania. Zaproponowano samoorganizujacy się system agentowy do wspierania decyzji handlowych. System bazując na glosowaniu z dynamicznymi wagami, wskazuje efektywne indykatory na podstawie ich poprzednich osiągnięć. Przedstawiono analizę formalną i wyniki weryfikacji, potwierdzającej cechy rozwiązania.
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Smart Document-Centric Processing of Human Oriented Information Flows
PublikacjaUsually people prefer to focus on creative rather than repetitive and schematic work patterns. Still, they must spend a lot of time complying with the procedures, selecting the information they receive and repeatedly restoring the previous state of work. This paper proposes the Mobile INteractive Document architecture (MIND) - a document-centric uniform interface to provide both effective communication of content and coordination...
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Simulating Malware with MAlSim
PublikacjaThis paper describes MAlSim - Mobile Agent Malware Simulator - a mobile agent framework developed to address one of the most important problems related to the simulation of attacks against information systems i.e. the lack of adequate tools for reproducing behaviour of malicious software (malware). The framework can be deployed over the network of an arbitrary information system and it aims at simulating behaviour of each instance...
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Simulating malware with MAlSim
PublikacjaThis paper describes MAlSim - Mobile Agent Malware Simulator - a mobile agent framework developed to address one of the most important problems related to the simulation of attacks against information systems, i.e. the lack of adequate tools for reproducing behaviour of malicious software (malware). The framework can be deployed over the network of an arbitrary information system and it aims at simulating behaviour of each instance...
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The Influence of the Co-Dopant Dexamethasone Phosphate on the Electrodeposition Process and Drug-Release Properties of Polypyrrole-Salicylate on Iron
PublikacjaIn this work, the influence of incorporation of two anti-inflammatory drugs dexamethasone phosphate and sodium salicylate on the electrodeposition process of polypyrrole (PPy) film on iron has been studied. The incorporation of the agents into PPy has been carried out in a one-step electropolymerization process on oxidizable iron. The role of each drug agent during the deposition process has been discussed. The morphological and...
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Chitosan, Collagen and Gelatin in the design of novel materials with antimicrobial acticity
PublikacjaMedical devices containing and releasing antiinfective agents directly on the site of injury are a common group of materials available and widely used in treating difficult to heal wounds. Sustained contact of the active agent to the damaged tissue, needed to inhibit infection and preservation of microbiological purity of the wound, is provided by the immobilization antimicrobial agents on the surface of the matrix material or...