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Wyniki wyszukiwania dla: multifunctional tacrine analogues, tacrine hybrids, alzheimer's disease, cholinergic transmission, neuroprotective activity, hepatoprotection.
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Therapeutic Potential of Multifunctional Tacrine Analogues
PublikacjaTacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this, analogues of tacrine are considered as a model inhibitor of cholinesterases in the therapy of Alzheimer’s disease. The interest in these compounds is mainly related to a high variety of their structure and biological properties. In the present review, we...
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Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
PublikacjaThe aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant,...
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Synthesis and Cholinesterase Inhibitory Activity of N-Phosphorylated /N-Tiophosphorylated Tacrine
PublikacjaNovel phosphorus and thiophosphorus tacrine derivatives were designed, synthesized and their biological activity and molecular modeling was investigated as a new potential anti-Alzheimer's disease (AD) agents. All new synthesized compound exhibited lower toxicity against neuroblastoma cell line (SH-SY5Y) in comparison with tacrine. Two analogues in the series, 7 and 9, demonstrated lack of cytotoxicity against hepatocellular cells...
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SYNTHESIS OF PHOSPHORUS TACRINE ANALOGUES AS A NEW POTENTIAL ANTI-ALZHEIMER’S DISEASE AGENTS
PublikacjaA series of novel phosphorus tacrine derivatives was obtained in three steps, including synthesis of 9-chlorotacrine, connection of 9-chlorotacrine with hexamethylenediamine, 1,8-diaminooctane and 1,12-diaminododecane linkers and reaction of obtained tacrine diamine analogues with corresponding acid ester to give nine tacrine organophosphorus compounds. All of the obtained final structures were characterized by 1H NMR, 13C NMR,...
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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
PublikacjaIn 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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Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublikacjaAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
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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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A Multifunctional Microwave Filter/Sensor Component Using a Split Ring Resonator Loaded Transmission Line
PublikacjaThis research is focused on the design and realiza2 tion of a microwave component with multifunctional filter/sensor 3 operation using a resonator-loaded transmission line (TL). It is 4 shown that while the structure acts as a bandstop filter, the 5 phase of the reflection coefficient from the loading resonator(s) 6 on a movable layer can be used for displacement sensing, thus 7 allowing for combining filtering with sensing in...
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Are advanced glycation end-products specific biomarkers for Alzheimer's disease?
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Vitamin D receptor gene polymorphisms in Alzheimer's disease patients
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Knowledge representation of motor activity of patients with Parkinson’s disease
PublikacjaAn approach to the knowledge representation extraction from biomedical signals analysis concerning motor activity of Parkinson disease patients is proposed in this paper. This is done utilizing accelerometers attached to their body as well as exploiting video image of their hand movements. Experiments are carried out employing artificial neural networks and support vector machine to the recognition of characteristic motor activity...
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The neuroprotective activity of new phenylalanine-based AMPA receptor antagonists
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Investigating the disease‐modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
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Tackling Alzheimer's disease: Hypothetical synergism between anti-inflammatory and anti-diabetic agents
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Anthracenedione analogues - synthesis and biological activity
PublikacjaW artykule opisano syntezę i aktywność biologiczną analogów antracenedionowych.
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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublikacjaA number of monocyclic SFTI-1 analogues modified in the conserved inhibitor P1 position by Pro, its L-hydroxyproline (Hyp) derivative as well as mimetics with different ring size were synthesized by the solid-phase method. Replacement of Ser6 by Pro, Hyp, and a four-member ring, L-azetidine-2-carboxylic acid (Aze), retained trypsin or chymotrypsin inhibitory activity. The determined association equilibrium constants of these analogues...
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Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity
PublikacjaEight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and oneof the three antimicrobials — ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) — were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the “click chemistry” method. This novel approach is reported here...
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Biological activity of tuftsin and its two analogues
PublikacjaPrzedstawiono badania, których celem była ocena wpływu analogów tuftsyny na żywotność mononuklearnych komórek krwi obwodowej (PBMC), limfocytów krwi obwodowej (PBL) i monocytów, ocena wpływu sekrecji czynnika martwicy nowotworu alfa (TNF) i interleukiny 6 (IL6) oraz zbadanie wpływu badanych związków na cytotoksyczność nuturalnych komórek zabójczych (NK).
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Phenylalanine-Based AMPA Receptor Antagonist as the Anticonvulsant Agent with Neuroprotective Activity—In Vitro and In Vivo Studies
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Safety-based approach in multifunctional building design
PublikacjaABSTRACT: The modern trend in design of the public buildings is to create multifunctional environments in one building, hosting a variety of functions. Multifunctional buildings entertain large number of visitors. The complexity and vulnerability of this type of public space are the main reasons to use within their design process the performance based approach including the recognition of hazards. Safety and reliability approach...
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Neuroprotective Effect of SGLT2 Inhibitors
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Structure-activity relationship studies on the antimicrobial activity of novel edeine a and d analogues
PublikacjaOpisano syntezę 4 nowych analogów peptydowego antybiotyku, edeiny a i d z wykorzystaniem klasycznej syntezy w roztworze. Stosowano metodę estrów aktywnych oraz metodę azydową do tworzenia wiązań peptydowych. Zbadano także aktywność przeciwgrzybową i przeciwbakteryjną opisanych połączeń.
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublikacjaIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Multifunctional Bandpass Filter/Displacement Sensor Component
PublikacjaThis paper presents the design and realization of a multifunctional bandpassfilter/displacement-sensor using an edge-coupled microstrip bandpass filter loaded by a pair of split ring resonators (SRRs). It is shown that while the structure acts as a bandpass filter at its operating frequency, the phase of the reflection coefficient from a movable loading resonator at the resonance frequency of the resonator can be used for displacement...
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Synthetic analogues of cyanobacterial alkaloid cylindrospermopsin and their toxicological activity
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new analogues of agmatine with higher activity to imidazoline receptors
PublikacjaOpracowano syntezę nowych pochodnych imidazoliny, będących kompilacją struktury agmatyny i imidazoliny w wyniku zaprojektowanej przez nas drogi syntezy. Kluczowymi substratami w syntezie były pochodne 1,2,4 -triaminobutanu, otrzymane z chronionego kwasu glutaminowego. Otrzymane nowe pochodne imidazoliny wykazywały zróżnicowane powinowactwo do receptorów imidazolinowych I1, I2 oraz do receptorów alfa -adrenergicznych.
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MULTI-CRITERIA MODEL IN MULTIFUNCTIONAL BUILDING SYSTEM DESIGN PROCESS
PublikacjaThe paper presents a multi-criteria approach in multifunctional building system design process. The aim is to develop a theory relative to the engineering system of multifunctional with a mathematical representation defined by a holistic network for the lifecycle of the designed object. The idea of work was to define the structure of a complex system. Background for the presented field is to develop a design strategy for multifunctional...
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Multi-Criteria Approach in Multifunctional Building Design Process
PublikacjaThe paper presents new approach in multifunctional building design process. Publication defines problems related to the design of complex multifunctional buildings. Currently, contemporary urban areas are characterized by very intensive use of space. Today, buildings are being built bigger and contain more diverse functions to meet the needs of a large number of users in one capacity. The trends show the need for recognition of...
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RESIDENTIAL FUNCTION IN MULTI-CRITERIA MULTIFUNCTIONAL BUILDING SYSTEM DESIGN PROCESS
PublikacjaThe paper presents the multi-criteria approach in the design process of residential structure as a part of a multifunctional building system. The purpose of work was to broaden the field of multifunctional building system design process. Background for the presented work is to define the direction of architectural growth of the modern city center area where actually are built complex and large capacity structures with a great impact...
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Analogues of trypsin inhibitor SFTI-1 modified in the conserved P1′ position by synthetic or non-proteinogenic amino acids retain their inhibitory activity
PublikacjaA series of linear and monocyclic (with a disulfide bridge only) analogues of trypsin inhibitor SFTI-1 modified in the P-1 and/or P-1' positions were synthesized by the solid-phase method. In the substrate specificity P-1 position, Phe or N-benzylglycine (Nphe) were introduced, whereas the conserved Ser6 in Bownam-Birk (BBI) inhibitors was replaced by Hse (L-homoserine), Nhse [N-(2-hydroxyethyl)glycine], Sar, and Ala. Kinetic studies...
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Contemporary multifunctional buildings towards a sustainable development of the housing environment
PublikacjaDevelopment of contemporary urban centers depends on the basis that buildings present more and more complex structures in terms of size and purpose. They are referred to as multifunctional buildings. This aspiration has its origins in the development of urban centers and in the desire to optimize the built-up areas. The article presents the theory of the approach to the design of multifunctional buildings with a focus on the residential...
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Selected biologic markers of inflammation and activity of Crohn’s disease
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Antifungal activity of thionated analogues of nva-fmdp and lys-nva-fmdp
Publikacjaotrzymano dwa peptydy w których wiązanie amidowe łączące aminokwasy zamieniono na tioamidowe w wyniku kilkunastoetapowej syntezy chemicznej. do reakcji tionowania zastosowano odczynnik lawessona. otrzymane związki poddano badaniom aktywności z wykorzystaniem pięciu szczepów candida , w tym szczepów opornych na flukonazol. stwierdzono, ze obecniość wiązania tioamidowego znacznie obniża aktywność przeciwgrzybową testowanych związków...
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Synthesis and Biological Activity of Strongly Fluorescent Tricyclic Analogues of Acyclovir and Ganciclovir
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Fluorescent Tricyclic Analogues of Acyclovir and Ganciclovir. A Structure−Antiviral Activity Study
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Combretastatin A-4 (CA-4) and its analogues. Synthesis and biological activity
PublikacjaSpośród wielu związków przeciwnowotworowych otrzymanych w ostatnich dwóch dekadach, na szczególną uwagę zasługują te, które powodują reorganizację mikrotubul. Jedną z takich substancji jest opisana w artykule kombretastatyna A-4 (CA-4), związek który indukuje apoptozęproliferujących komórek śródbłonka naczyń guza nowotworowego. Hamuje on polimeryzację tubuliny, prowadząc do rozpadu mikrotubul. CA-4 wyizolowana została z kory wierzby...
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The Bactericidal Activity of Temporin Analogues Against Methicillin Resistant Staphylococcus aureus
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Molecular features of thymidine analogues governing the activity of human thymidine kinase
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Professional activity, gender and disease-related emotions: The impact on parents' experiences in caring for children with phenylketonuria
PublikacjaIntroduction: Clinical management of rare diseases often fails to acknowledge the challenges faced by caregivers.Whilst management of phenylketonuria (PKU) may not be considered as dire as other conditions, most studiesprimarily concentrate on clinical issues, dietary adherence, or the quality of life of the PKU patients, leavingcaregivers in the background. The aim of the study was to evaluate the psychosocial...
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Structure activity relationship for a series of peptidomimetic antimicrobial prodrugs containing glutamine analogues.
PublikacjaZbadano specyficzność transporterów Dpp i Opp w stosunku do peptydów zawierających FMDP. Przy pomocy modelowania cząsteczkowego zaproponowano najbardziej prawdopodobne struktury konformerów peptydów i skorelowano je z aktywnością przeciwbakteryjną oraz specyficznością transporterów peptydowych.
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Genetic predisposition to inflammatory bowel disease
PublikacjaInflammatory bowel disease (IBD) is a chronic, incurable inflammatory disease of the digestive system. The two main disease entities included in the IBD are ulcerative colitis and Crohn's disease. According to epidemiological studies there are more and more new cases every year. In especially among the youngest patients with symptoms of malnutrition and growth inhibition to land up in hospitalwith cancer suspected. The purpose...
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Topological extraordinary optical transmission
PublikacjaΤhe incumbent technology for bringing light to the nanoscale, the near-field scanning optical microscope, has notoriously small throughput efficiencies of the order of 10^4-10^5 or less. We report on a broadband, topological, unidirectionally guiding structure, not requiring adiabatic tapering and, in principle, enabling near-perfect (∼100%) optical transmission through an unstructured single arbitrarily subdiffraction slit at...
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Cytotoxic and Antioxidant Activities of Benzohydroxamic Acid Analogues
Publikacja20 benzohydroxamic acid analogues were synthesized and evaluated for their in vitro cytotoxicities against mouse mammary tumor cells as well as antioxidant activities against DPPH radical and superoxide anion. It was found that benzothiohydroxamic acids exhibit greater cytotoxicities than benzohydroxamic acids and N-isopropyl derivatives are more active than N-methyl ones. On the other hand, benzothiohydroxamic acids show more...
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Antimicrobial Activity of Chimera Peptides Composed of Human Neutrophil Peptide 1 (HNP-1) Truncated Analogues and Bovine Lactoferrampin
PublikacjaThree chimera peptides composed of bovine lactoferrampin and the analogue of truncated human neutrophil peptide 1 were synthesized by the solid-phase method. In two compounds peptide chains were connected via isopeptide bond, whereas in the third one disulfide bridge served as a linker. All three chimeras displayed significantly higher antimicrobial activity than the constituent peptides as well as their equimolar mixtures. The...
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Efficient synthesis of PMMA@Co0.5Ni0.5Fe2O4 organic-inorganic hybrids containing hyamine 1622 – Physicochemical properties, cytotoxic assessment and antimicrobial activity
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Mathematical Modelling of Drive System with an Elastic Coupling Based on Formal Analogy between the Transmission Shaft and the Electric Transmission Line
PublikacjaIn the paper, the kinematic structure of the transmission shaft between the driving motor and the working mechanism is studied. The analysis is based on electrical and mechanical similarities. The equivalent circuits, typical for electrical systems, are defined for the transmission shaft concerned. Modelling of the transmission shaft based on a formal analogy between the transmission shaft and the electric transmission line is...
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Cooperative Data Transmission in Wireless Vehicular Networks
PublikacjaThe paper presents issues related to the cooperative transmission in wireless vehicular networks. Cooperative transmission involves the use of mobile terminals as relay stations to improve the transmission quality, improve network performance and reduce energy consumption. The paper presents the methods used to implement cooperative transmission and the types of cooperative networks.
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Computational Fluid Dynamic study on the wind characteristics of a multifunctional building system model in developed coastal cities
PublikacjaThis paper presents an approach for providing innovative technology by applying fluid mechanics to the field of architectural design. The aim is to make a building’s shape profitable and strengthen environmental protection by using the wind force to create an integrated wind absorption definition for a multifunctional building system model. Furthermore, taking control of the wind flow over an object can have an impact on not only...
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Synthesis, biological activity and conformational analysis of head-to-tail cyclic analogues of LL37 and histatin 5
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Transmission parameters of underwater communication channels
PublikacjaThe underwater environment is tough and demanding as a communication channel for ultrasonic signals. The channel transmission characteristics in marine and inland waters depend much on local bathymetry and changing weather conditions. The architecture and performance of a reliable underwater acoustic communication (UAC) system should allow real-time adaptation of its transmission parameters to a large variety of possible channel...