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Wyniki wyszukiwania dla: MIC, ANTIMICROBIAL ACTIVITY, MURAMYL DIPEPTIDE DERIVATIVES, ANALOGUES OF ANTHRAQUINONES, RETRO-TUFTSIN DERIVATIVES
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Chlorophylls and their Derivatives Used in Food Industry and Medicine
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Affinity of fentanyl and its derivatives for the σ1-receptor
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Thermodynamics of new piroxicam derivatives in terahertz light
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Glycyrrhetinic acid and its derivatives in infectious diseases
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Fractional Derivatives Application to Image Fusion Problems
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Chromogenic macrocyclic derivatives of azoles - synthesis and properties,
PublikacjaNew azocrown ethers comprising imidazoles in the macrocycle have been synthesized. Imidazole, 2-methyl-, 4-methyl-, and 4-phenylimidazole were incorporated to form macrocyclic units by coupling with the appropriate bis-diazonium salts. The syntheseswere performed under high dilution conditions. The X-ray structure of a water adduct of the 21-membered crown ether derivative of 4-methylimidazole 8 has been solved. Metal...
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Synthetic genistein derivatives as modulators of glycosaminoglycan storage
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Chromogenic Macrocyclic Derivatives of Azoles - Synthesis and Properties
PublikacjaOpisano syntezę makrocyklicznych azokoron zawierających resztę pirolu i imi-dazolu w makropierścieniu. Zbadano zdolność kompleksowania kationów metaliprzez otrzymane związki makrocykliczne przy pomocy spektrofotometrii UV-Visw acetonitrylu. Zbadano także właściwości jonoforowe związków w membranowychelektrodach jonoselektywnych. Ustalono strukturę krystalograficzną 18-czło-nowej pochodnej pirolu.
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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery
PublikacjaAbstract: Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently...
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Antiproliferative activity of anthraquinones determined by clonogenic assay
Dane BadawczeThe data contains the colony formation analysis in A549, H460 and H226 cells after exposure to TXT2 and TXT4. DMSO was used as a negative control.
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublikacjaThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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Photoresponsive Amide-Based Derivatives of Azobenzene-4,4′-Dicarboxylic Acid—Experimental and Theoretical Studies
PublikacjaAzobenzene derivatives are one of the most important molecular switches for biological and material science applications. Although these systems represent a well-known group of compounds, there remains a need to identify the factors influencing their photochemical properties in order to design azobenzene-based technologies in a rational way. In this contribution, we describe the synthesis and characterization of two novel amides...
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Synthesis of phosphono and phosphate derivatives of hydroxyimino-D-alditols as new potential antifungal agents
PublikacjaIn search for new effective we antyfungals we focus on two enzymes involved in biosynthesis of the fungal cell wall. The first enzyme is glucosamine-6-phosphate (GlmS), which catalyzes transformation of D-fructose-6-phosphate (Fru-6P) to D-glucosamine-6-phodphate (GlcN-6P) in the chitin biosynthesis pathway. The second enzyme is phosphomannose isomerase (PMI) repored to play a crucial role in biosynthesis of many mannosylated structures,...
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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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Synthetic analogues of cyanobacterial alkaloid cylindrospermopsin and their toxicological activity
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Analysis of the influence of polystyrene microplastics and their derivatives on the DNA of human colon epithelial cells HT29 with the comet assay
PublikacjaWe have been using plastic for almost a century and nowadays a lot of them circulates as pollutants in the environment and still defragmenting to micro and nanoscale. The exposition through the food chain and its precise impact on human health is still not clear. In our study, we tested real food packaging after contact with food products and real thermoinsulation and environmental samples of polystyrene in different model liquids,...
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The immunological properties, cytotoxic effect and antimicrobial activities of novel analogues of edeine antibiotics
PublikacjaOpisano syntezę kilku nowych analogów edein a i d z zastosowaniem klasycznych metod syntezy peptydów w roztworze oraz przedstawiono wyniki badań cytotoksycznych na kilku liniach komórek ludzkich oraz wyniki badań mikrobiologicznych w stosunku do bakterii gramododatnich i gramoujemnych. Opisano również wyniki badań immunologicznych na modelu myszy.
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Amberlyst-15 catalysed synthesis of novel indole derivatives under ultrasound irradiation: Their evaluation as serotonin 5‑HT2C receptor agonists
PublikacjaA series of indole based novel Schiff bases was designed as potential agonists of 5‑HT2C receptor that was supported by docking studies in silico. These compounds were synthesized via Amberlyst-15 catalysed condensation of an appropriate pyrazole based primary amine with the corresponding indole-3-aldehyde under ultrasound irradiation at ambient temperature. A number of target Schiff bases were obtained...
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Photodynamic Inactivation of Bacteria with Porphyrin Derivatives: Effect of Charge, Lipophilicity, ROS Generation, and Cellular Uptake on Their Biological Activity In Vitro
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Preliminary Investigation of the Antibacterial Activity of Antitumor Drug 3-Amino-1,2,4-Benzotriazine-1,4-Dioxide (Tirapazamine) and its Derivatives
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Peptide dendrimers as antifungal agents and carriers for potential antifungal agent—N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐ diaminopropanoic acid—synthesis and antimicrobial activity
PublikacjaA series of peptide dendrimers and their conjugates with antimicrobial agent FMDP (N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐diamino‐propanoic acid) were synthesized. The obtained compounds were tested for the antibacterial and antifungal activity. All novel dendrimers displayed much better activity against the tested strains than FMDP itself. Moreover, their conjugates with FMDP also exhibited antimicrobial activity. The most promising molecules...
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Meldrum’s acid assisted formation of tetrahydroquinolin‑2‑one derivatives a short synthetic pathway to the biologically useful scaffold
PublikacjaA new method for the preparation of tetrahydroquinolin-2-one derivatives is presented. This approach involves a two-step reaction between enaminones and acylating agents, immediately followed by electrophilic cyclization, all within a single synthesis procedure, eliminating the need to isolate intermediates. The entire process is facilitated by the use of acyl Meldrum’s acids which not only shortens the preparation time of the...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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IKE1-IKE3 (C-1305 derivatives) inhibitory effect of the Yeast Topoisomerase II relaxation activity
Dane BadawczeInhibition of Yeast Topoisomerase II were analyzed according to relaxation assay kit from Inspiralis. Briefly, 250 ng of supercoiled pBR322 DNA, 1 mM ATP, 1-200 μM of analyzed compound were mixed with reaction buffer (1 mM Tris-HCl (pH 7.9), 10 mM KCl, 0.5 mM MgCl 2, 0.2 % (v/v) glycerol). The reaction was initiated by the addition of an enzyme, allowed...
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Composition and antimicrobial activity of fatty acids detected in the hygroscopic secretion collected from the secretory setae of larvae of the biting midge Forcipomyia nigra (Diptera: Ceratopogonidae)
PublikacjaThe hygroscopic secretion produced by the secretory setae of terrestrial larvae of the biting midge Forcipomyia nigra (Winnertz) was analysed using gas chromatography coupled with mass spectrometry (GC-MS). The viscous secretion is stored at the top of each seta and absorbs water from moist air. GC-MS analyses (four independent tests) showed that the secretion contained 12 free fatty acids, the most abundant of which were oleic...
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One-Step Synthesis of b-Lactams with Retro-Amide Side Chain
PublikacjaAbstract: A one pot synthesis for preparation of 1,4-disubstituted-2-oxo-azetidine-3-carboxylic acid amides was developed. 5-(α-N-substituted-amino-α'-hydroxy)methylene Meldrum's acids act as a source of ketenes that react with aldimines in boiling toluene to give b-lactams with retro-amid side chain.
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Ewa Augustin dr hab.
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Hydrophilic Films Based on Carboxymethylated Derivatives of Starch and Cellulose
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Emulsion-Based Gel Loaded with Ibuprofen and Its Derivatives
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The photophysics of β-homo-tyrosine and its simple derivatives
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Photophysical and theoretical studies of diphenylacetylene derivatives with restricted rotation
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Synthesis of Thermally Stable Energetic 1,2,3-Triazole Derivatives
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Functionalization of cysteine derivatives by unsymmetrical disulfide bond formation
PublikacjaOpracowano metodę funkcjonalizacji pochodnych cysteiny przy pomocy tworzenia niesymetrycznego wiązania disulfidowego. Opracowana metoda okazała się bardzo łagodna, wydajna, i niewrażliwa na obecność dodatkowych grup funkcyjnych.
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Microwave-assisted synthesis of zinc derivatives of potato starch
PublikacjaZincatated potato starch was prepared in a solid-state, microwave-assisted reaction using generated in situ sodium tetrahydroxozincate [Na2Zn(OH)4]. For comparison, zincatation of starch was also carriedout on convectional heating. Depending on the irradiation conditions, the products of either mono- or crosslinking esterification were formed. Higher power applied at shorter exposition offered products ofmonoesterification, and...
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Electron ionization induced fragmentation of fluorinated derivatives of bisphenols
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Hydration of urea and its derivatives - Volumetric and compressibility studies
PublikacjaThe densities and sound velocities at T = (288.15, 293.15, 298.15, 303.15 and 308.15) K have been measured for aqueous solutions of urea, N,N-dimethylurea, N,N-diethylurea, N-propylurea, N-butylurea. From these data the apparent molar volumes, V the apparent molar isentropic compressions, KS,, and the Passynski solvation numbers of solutes have been determined. The concentration dependencies of the calculated quantities, their...
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Efficient synthesis of orthogonally protected spermidine and norspermidine derivatives
PublikacjaOtrzymano kilka chronionych pochodnych spermidyny i norspermidyny w wyniku reakcji cyjanoetylowania chronionych diamin, ochrony drugorzędowej grupy aminowej oraz redukcji otrzymanego nitrylu za pomocą wodorku litowo-glinowego w temperaturze 0° C.
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Copper(I) iodide ribbons coordinated with thiourea derivatives
PublikacjaTwo products of the reactions of CuI with 1-benzoyl-3-(4-bromophenyl)thiourea and with 1-benzoyl-3-(2-iodophenyl)thiourea have been obtained and characterized, namely poly[[[1-benzoyl-3-(4-bromophenyl)thiourea-κS]-µ3-iodidocopper(I)] acetone hemisolvate], {[CuI(C₁₄H₁₁BrN₂OS)]‧0.5C₃H₆O}ₙ, and poly-[µ₄-iodido-µ₃-iodido-[N-(benzo[d]thiazol-2-yl)benzamide-κN]dicopper(I)], [Cu₂I₂(C₁₄H₁₀N₂OS)]ₙ. Their structures, determined by single-crystal...
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Hedging Strategies of Derivatives Instruments for Commodity Trading Entities
PublikacjaHedging as an outcome of risk management arises to account several questions. Mentioned aspect of size of the hedging is one of them. Latter questioning refers to whether producer of manufacturer are willing to secure entire exposure, when the hedging should start, now or later in the future, what is the vision on market like direction of market, time of interest, magnitude of exposure, what would be the preferred instruments of...
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Densimetric and ultrasonic characterization of urea and its derivatives in water
PublikacjaW oparciu o pomiary gęstości dla serii roztworów jak i rozpuszczalnika wykonanych w temperaturach 15, 20, 25, 30 i 35oC wyznaczono pozorne molowe objętości mocznika, N-metylomocznika, N,N'-dimetylomocznika, N,N,N',N'-tetrametylomocznika, N-etylomocznika, N,N'-dietylomocznika jak i N-butylomocznika w wodzie. Dodatkowe pomiary szybkości dźwięku przeprowadzone w temperaturze 25oC pozwoliły obliczyć ściśliwości adiabatyczne, pozorne...
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Do Phenyl Substituents Affect the Properties of Azobenzocrown Derivatives?
PublikacjaNew products of photo- and thermal rearrangements of 19-membered azoxybenzocrown with phenyl substituents in benzene rings in the para positions to oligooxyethylene fragments are characterized. The yields of photochemical transformations depend on the solvent. Para-hydroxyazocrown is formed with yields over 50% in propan-2-ol. Ortho-hydroxyazobenzocrown is obtained with yields up to 70% in toluene/acetic acid mixture. Macrocyclic...
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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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Pharmacological Classification and Activity Evaluation of Furan and Thiophene Amide Derivatives Applying Semi-Empirical ab initio Molecular Modeling Methods
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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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Analysis of bisphenols and their derivatives in infant and toddler ready-to-feed milk and powdered milk by LC MS/MS
PublikacjaReady-to-feed milk and powdered milk packed in different types of packaging lined with resin are chosen as the primary or complementary diet for infants and toddlers. An HPLC–MS/MS method was established and validated for the determination of nineteen bisphenols and their derivatives in such samples. The recoveries were from 31% to 120%, while the values of limit of detection and quantification were in the range of 0.24–0.40 and...
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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
PublikacjaNew 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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Ultrasound assisted synthesis of 3-alkynyl substituted 2-chloroquinoxaline derivatives: Their in silico assessment as potential ligands for N-protein of SARS-CoV-2
PublikacjaIn view of recent global pandemic the 3-alkynyl substituted 2-chloroquinoxaline framework has been explored as a potential template for the design of molecules targeting COVID-19. Initial in silico studies of representative compounds to assess their binding affinities via docking into the N-terminal RNA-binding domain (NTD) of N-protein of SARS-CoV-2 prompted further study of these molecules. Thus building of a small library of...
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Efficient Gradient-Based Algorithm with Numerical Derivatives for Expedited Optimization of Multi-Parameter Miniaturized Impedance Matching Transformers
PublikacjaFull-wave electromagnetic (EM) simulation tools have become ubiquitous in the design of microwave components. In some cases, e.g., miniaturized microstrip components, EM analysis is mandatory due to considera¬ble cross-coupling effects that cannot be accounted for otherwise (e.g., by means of equivalent circuits). These effects are particularly pronounced in the structures in¬volving slow-wave compact cells and their numerical...
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Chemical reactivity and antimicrobial activity of N-substituted maleimides
PublikacjaZsyntezowano kilkanaście N-podstawionych maleimidów, zawierających w swojej strukturze podstawniki o różnej wielkości i polarności.Maleimidy o charakterze obojętnym wykazywały silny efekt przeciwgrzybowy; ich aktywność przeciwbakteryjna była zróżnicowana. Niską aktywność przeciwbakteryjną, ale wysoką aktywność cytostatyczną stwierdzono dla maleimidów o charakterze zasadowym. Reaktywność chemiczna i lipofilowość miały wpływ na aktywność...
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Chemical Composition and Antimicrobial Activity of New Honey Varietals
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