Wyniki wyszukiwania dla: XANTHINE OXIDASE INHIBITORS
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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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Structure-activity relationship study of tetrapeptide inhibitors of the Vascular Endothelial Growth Factor A binding to Neuropilin-1
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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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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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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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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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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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Separate synthesis and evaluation of glucitol bis-phosphate and mannitol bis-phosphate, as competitive inhibitors of fructose bis-phosphate aldolases
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Discussion on 3-hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors reduce human pancreatic cancer cell invasion and metastasis
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Screening of potential inhibitors for COVID-19 main protease from phytoconstituents of Tectona grandis Linn: application of molecular modeling studies
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Changes in Gene and Protein Expression of Metalloproteinase-2 and -9 and Their Inhibitors TIMP2 and TIMP3 in Different Parts of Fluoride-Exposed Rat Brain
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Glucosylceramide Mimics: Highly Potent GCase Inhibitors and Selective Pharmacological Chaperones for Mutations Associated with Types 1 and 2 Gaucher Disease
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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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Do not die, become senescent: a new type of cellular resistance induced by topoisomerase II inhibitors in tumor cells with functional p53
PublikacjaJednym z efektów wywoływanych przez związki przeciwnowotworowe w komórkach nowotworowych jest trwałe zahamowanie wzrostu, związane z pojawieniem się markerów procesu starzenia komórkowego. Proponuje się, że może to być nowy sposób na zahamowanie postępu choroby nowotworowej. W naszych badaniach wykazujemy, że zahamowanie wzrostu indukowane przez związki z grupy inhibitorów topoizomerazy II w komórkach raka płuc A549 jest związane...
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Trypsin inhibitors from the garden four o’clock (Mirabilis jalapa) and spinach (Spinacia oleracea) seeds: Isolation, characterization and chemical synthesis
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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublikacjaBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Microbial acetylcholinesterase inhibitors for Alzheimer’s therapy: recent trends on extraction, detection, irradiation-assisted production improvement and nano-structured drug delivery
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Meat Proteins as Dipeptidyl Peptidase IV Inhibitors and Glucose Uptake Stimulating Peptides for the Management of a Type 2 Diabetes Mellitus In Silico Study
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Efficacy of high-dose corticosteroid-based treatment for chronic lymphocytic leukemia patients with p53 abnormalities in the era of B-cell receptor inhibitors
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Selection of peptomeric inhibitors of bovine α-chymotrypsin and cathepsin G based on trypsin inhibitor SFTI-1 using a combinatorial chemistry approach
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Synthesis, anticandidal activity of N3-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives – Novel inhibitors of glucosamine-6-phosphate synthase
PublikacjaNovel FMDP amiders 4-6 have been synthesized and tested against Candida strains. The anticandidal activity has been confined only to Candida albicans. Anticandidal activity of the tested amides has correlated with their inhibitory activity of glucosamine-6-phosphate synthase in cell free extract from Candida albicans.
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublikacjaA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM)
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A. Computational analysis by molecular docking of thirty alkaloid compounds from medicinal plants as potent inhibitors of SARS-CoV-2 main protease(2020).
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Experimental and Machine-Learning-Assisted Design of Pharmaceutically Acceptable Deep Eutectic Solvents for the Solubility Improvement of Non-Selective COX Inhibitors Ibuprofen and Ketoprofen
PublikacjaDeep eutectic solvents (DESs) are commonly used in pharmaceutical applications as excellent solubilizers of active substances. This study investigated the tuning of ibuprofen and ketoprofen solubility utilizing DESs containing choline chloride or betaine as hydrogen bond acceptors and various polyols (ethylene glycol, diethylene glycol, triethylene glycol, glycerol, 1,2-propanediol, 1,3-butanediol) as hydrogen bond donors. Experimental...
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Hydrophobic derivatives of 2-amino-2-deoxy-D-glucitol-6-phosphate: a newtype of D-glucosamine-6-phosphate synthase inhibitors with antifungal action.
PublikacjaDokonano syntezy szeregu N-acylowych i estrowych pochodnych 2-amino-2-deok-sy-glucitolo-6-fosforanu (ADGP) i zbadano ich aktywność przeciwgrzybową oraz wobec enzymów zaangażowanych we wczesne etapy biosyntezy chityny w komórkach grzybów. Wszystkie badane pochodne okazały się słabszymi inhibitorami enzymu syntezy GlcN-6-P aniżeli ADGP, ale niektóre z nich wykazywały znacznie wyższą aktywność przeciwgrzybową niż związek macierzysty....
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Efficacy and safety of B-cell receptor signaling pathway inhibitors in relapsed/refractory chronic lymphocytic leukemia: a systematic review and meta-analysis of randomized clinical trials
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Exploiting the S4–S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis
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Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors
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Novel isatin–indole derivatives as potential inhibitors of chorismate mutase (CM): their synthesis along with unexpected formation of 2-indolylmethylamino benzoate ester under Pd–Cu catalysis
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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
PublikacjaA 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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Chromatographic analysis of extracts isolated from different poplar species as potential inhibitors of enzymatic hydrolysis Analiza chromatograficzna substancji ekstrakcyjnych pozyskanych z różnych odmian topoli jako potencjalnych inhibitorów hydrolizy enzymatycznej
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Antiviral activity of bee bread derived from polish apiaries.
Dane BadawczeBee bread is a product of fermentation of bee-collected pollen and revealed a high nutritional value. Other bee products, such as honey and propolis, are known for their antiviral activity, but bee bread is still under investigation, thus its antiviral potential is still unspecified. For investigation antiviral activity of bee bread samples, cytotoxicity...
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A. Computational analysis by molecular docking of thirty alkaloid compounds from medicinal plants as potent inhibitors of SARS-CoV-2 main protease(2020). Focused on analysis of the Medicinal plants that have potential therapeutic ability against COVID-19.
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Mateusz Brodowski
OsobyMateusz Brodowski received his engineer degree in 2019 at the of Chemical Technology with a specialization in Anti-Corrosion Protection Technologies, in his engineer thesis he examined the effectiveness of green corrosion inhibitors. He finished a Master's degree in the field of Mechatronics, realizing the work of creating software for data acquisition from the electrochemical measurement system. Since 2019, he has been working...
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Biobatteries and biofuel cells with biphenylated carbon nanotubes
PublikacjaSingle-walled carbon nanotubes covalently biphenylated are used for the construction of cathodes in a flow biobattery and in flow biofuel cell. Zinc covered with a hopeite layer is the anode in the biobattery and glassy carbon electrode covered with bioconjugates of single-walled carbon nanotubes with glucose oxidase and catalase is anode of the biofuel cell. The potentials of the electrodes are measured vs. the Ag/AgCl reference...
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The microstructure of AA5754 alloy under corrosion in alkaline media (pH=11) with 20 mM of various carboxylic acids
Dane BadawczeThis dataset contains scanning electron microscopy (SEM) micrographs taken for polished aluminum AA5754 alloy samples, exposed for 100 min in bicarbonate buffer (pH=11) with the addition of 20 mM of carboxylic acids, namely: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, tricarballylic acid and serine. The goal of this study was...
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The microstructure of AA5754 alloy under corrosion in alkaline media (pH=11) with 4.5 mM of various carboxylic acids
Dane BadawczeThis dataset contains scanning electron microscopy (SEM) micrographs taken for polished aluminum AA5754 alloy samples, exposed for 100 min in bicarbonate buffer (pH=11) with the addition of 4.5 mM of carboxylic acids, namely: citric acid, malic acid, maleic acid, succinic acid, tartaric acid, tricarballylic acid and serine. The goal of this study was...
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Extracting functional groups of ALLINI to design derivatives of FDA‐approved drugs: Inhibition of HIV‐1 integrase
PublikacjaHIV‐1 integrase (IN) is crucial for integration of viral DNA into the host genome and a promising target in development of antiretroviral inhibitors. In this work, six new compounds were designed by linking the structures of two different class of HIV‐1 IN inhibitors (active site binders and allosteric IN inhibitors (ALLINIs)). Among newly designed compounds, INRAT10b was found most potent HIV‐1 IN inhibitor considering different...
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Electrochemical investigations on corosivity of de-icing liquids for railway infrastructure
PublikacjaThe paper presents the results of electrochemical tests of the de-icing fluid for railway infrastructure. DC and AC electrochemical tests were performed to determine the corrosion rates of structural steel, cast iron and aluminium in the newly produced fluid. The results were compared with the corrosion rates of the same materials in the fluid without corrosion inhibitors. The obtained test results indicate a low corrosion risk...
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Amino Acid and Peptide‐Based Antiviral Agents
PublikacjaA significant number of antiviral agents used in clinical practice are amino acids, short peptides, or peptidomimetics. Among them, several HIV protease inhibitors (e. g. lopinavir, atazanavir), HCV protease inhibitors (e. g. grazoprevir, glecaprevir), and HCV NS5A protein inhibitors have contributed to a significant decrease in mortality from AIDS and hepatitis. However, there is an ongoing need for the discovery of new antiviral...
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Korozja w środowisku ropy naftowej. Czynniki i monitorowanie
PublikacjaPrzedstawiono analizy właściwości ropy naftowej z punktu widzenia zawartych w niej czynników korozyjnych oraz ich wpływu na korozję stali w trakcie procesu destylacji ropy naftowej. Krytycznej analizie poddane zostały możliwości oferowane przez współczesne techniki pomiarowe. Wskazano na istotność prowadzenia kompleksowego programu oceny ropy, monitorowania korozji oraz stosowania ochrony inhibitorowej w celu ochrony instalacji...
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Removal of phenolic inhibitor compounds from hydrolysates and post-fermentation broths by using a Hydrophobic Magnetic Deep Eutectic Solvent
PublikacjaHydroxymethylfurfural (HMF), furfural (FF), hydroquinone (HQ), and vanillin (VAN) are among the main inhibitors generated during most of biomass pre-treatments prior to fermentation processes. They are recognized as toxic to several fermentative microorganisms and therefore cause a decrease in biohydrogen or biofuel production (after hydrolysis). Moreover, if they are released into aqueous solutions (after fermentation), they can...
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Oxygen biosensor based on carbon nanotubes directly grown on graphitic substrate
PublikacjaFilms of carbon nanotubes were synthesized on the graphitic substrates by CVD method in the presence of catalyst. Two different catalysts were used, that is nickel and iron, supported on graphitic substrates. The as-obtained nanotubes were analyzed by SEM imaging with EDX and Raman spectroscopy. The results revealed their multi-walled morphology. Free radical reaction was carried out in order to chemically functionalize synthesized...