Wyszukiwarka
Wyniki wyszukiwania dla: SULFONAMIDE DERIVATIVES
-
Synthesis of Thermally Stable Energetic 1,2,3-Triazole Derivatives
Publikacja -
Synthesis of Thermally Stable Energetic 1,2,3‐Triazole Derivatives
Publikacja -
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.
-
The biological activity of new tuftsin derivatives - induction of phagocytosis
PublikacjaFagocytoza odgrywa ważną rolę w ochronie organizmu przed różnymi mikroorganizmami. Proces ten może być indukowany przez różne czynniki np. endogenny immunomodulator jakim jest tuftsyna czy muramylo-dipeptyd (MDP), najmniejszy syntetyczny glikopeptyd bakteryjnej ściany komórkowej. Zsyntetyzowano nowe analogi MDP i nor-MDP z tuftsyną i retro-tuftsyną, które są zdolne do indukowania fagocytozy. Najbardziej obiecujące okazały się dwa...
-
Amphotericin B and Its New Derivatives - Mode of Action
PublikacjaAmphotericin B (AmB) is a well known antifungal and antiprotozoal antibiotic used in the clinic for several decades. Clinicalapplications of AmB, however, are limited by its nephrotoxicity and many other acute side effects which are not acceptable by patientswhen their life is not threaten. In order to improve the therapeutic index of this drug, lipid formulations have been introduced and manyefforts have been made to obtain less...
-
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...
-
Biological activity of conjugates of muramyl dipeptides with batracylin derivatives
PublikacjaZaprezentowano immunomodulacyjne właściwości nowych koniugatów batracyliny (BAT) z pochodnymi muramylodipeptydów wobec subpopulacji leukocytów krwi obwodowej hodowanych w obecności komórek linii nowotworowych. Leukocyty izolowane były z krwi obwodowej uzyskanej od zdrowych ochotników. Zbadane koniugaty MDP lub nor-MDP z batracyliną wykazały silniejsze własności hamujące proliferację komórek wybranych linii nowotworowych (K562,...
-
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...
-
Acyl Meldrum's acid derivatives: application in organic synthesis
PublikacjaThis review is focused on one of the most important classes of Meldrum's acid derivatives commonly known as acyl Meldrum's acids. The preparation methods of these compounds are considered including the recently proposed and rather rarely used ones. The chemical properties of acyl Meldrum's acids are described in detail, including thermal stability and reactions with various nucleiophiles. The possible mechanisms of these transformations...
-
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...
-
Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublikacjaBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
-
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...
-
On Applications of Elements Modelled by Fractional Derivatives in Circuit Theory
PublikacjaIn this paper, concepts of fractional-order (FO) derivatives are reviewed and discussed with regard to element models applied in the circuit theory. The properties of FO derivatives required for the circuit-level modeling are formulated. Potential problems related to the generalization of transmission-line equations with the use of FO derivatives are presented. It is demonstrated that some formulations of FO derivatives have limited...
-
Biochemical, Structural Analysis, and Docking Studies of Spiropyrazoline Derivatives
PublikacjaIn this study, we evaluated the antiproliferative potential, DNA damage, crystal struc‐ tures, and docking calculation of two spiropyrazoline derivatives. The main focus of the research was to evaluate the antiproliferative potential of synthesized compounds towards eight cancer cell lines. Compound I demonstrated promising antiproliferative properties, especially toward the HL60 cell line, for which IC50 was equal to 9.4 μM/L....
-
Biological activity of conjugates of muramyl dipeptides with batracylin derivatives
PublikacjaW artykule opisano aktywność biologiczną koniugatów muramylo-dipeptydów z batracyliną lub pochodnymi batracyliny. Badania przeprowadzone w Akademii Medycznej w Gdańsku miały na celu oznaczenie immunomodulacyjnych właściwości tych koniugatów wobec subpopulacji leukocytów krwi obwodowej hodowanych w obecności komórek nowotworowych (K562, WEHI164, Ab melanoma). Leukocyty izolowane były z krwi obwodowej uzyskanej od zdrowych ochotników....
-
Nitrogen monitoring in atmospheric deposition and its removal from municipal and industrial wastewater
PublikacjaBadano zmiany stężenia azotu w opadach atmosferycznych oraz warunki usuwania azotu ze ścieków komunalnych i przemysłowych. Badano wpływ wybranych sulfonamidów na proces nitryfikacji oraz oznaczano ich stopień biodegradacji. Stwierdzono, że sulfonamidy są substancjami, które hamują procesy biologicznego oczyszczania ścieków, jak również w niskim stopniu ulegają biodegradacji.
-
The effect of anthraquinone derivatives on telomerase activity
Dane BadawczeThe data set contains images of the PCR products obtained from the Telomerase Repeated Amplification Protocol (TRAP). The effect of anthraquinone derivatives (TXT1-TXT9) on telomerase activity was comparatively examined using the following reference compounds: BIBR1532, TMPyP4 and mitoxantrone (MTX).
-
Synthesis and biological activity of mycophenolic acid-amino acid derivatives
Publikacja -
Synthesis of ester derivatives of propylene glycol in the presence of zinc carboxylates.
PublikacjaZbadano wpływ temperatury i stężenia karboksylanów cynku na przebieg estryfikacji glikolu propylenowego kwasami tłuszczowymi. Otrzymano emulgatory, w których maksymalne stężenie monoestru wynosiło 55-57%.
-
Umbilical and Placental Derivatives in Temporomandibular Joint Treatment: A Systematic Review
Publikacja -
Photophysics of 7-Hydroxytetrahydroisoquinoline-3-carboxylic Acid and Its Derivatives
Publikacja -
Supramolecular Interactions between β-Cyclodextrin and the Nucleobase Derivatives of Ferrocene
Publikacja -
Conjugation of polyethylenimine and its derivatives to carbon-encapsulated iron nanoparticles
Publikacja -
Natural composites based on polysaccharide derivatives: preparation and physicochemical properties
Publikacja -
Prediction of antimicrobial activity of imidazole derivatives by artificial neural networks
Publikacja -
Alkylation of 9-substituted guanine derivatives with α,ω-dihaloalkanes
Publikacja -
Studies on the influence of β-cyclodextrin derivatives on the physical stability of famotidine
PublikacjaThe usage of Fourier transform infrared spectroscopy, near infrared spectroscopy, differential scanning calorimetry and microscopy is presented in this work focused on the exploration of the effect of CD on the physical stability of famotidine (FAM). The most significant information was achieved by analysis of the second derivatives ofnear infrared (NIR) spectra recorded. Changes in the shape of spectra derivatives allow...
-
Curcumin Derivatives in Medicinal Chemistry: Potential Applications in Cancer Treatment
Publikacja -
The content of butyl- and phenyltin derivatives in the sediment from the Port of Gdansk
PublikacjaPróbki osadów portowych były pobierane dwukrotnie (2003 i 2005)z różnych nabrzeży w Porcie Gdańsk. Rdzenie o długości 25 cm były dzielone na warstwy o grubości 2 i 5cm i po odpowiednim przygotowaniu (w tym także analizie sitowej) były poddawane analizie na zawartość związkow cynoorganicznych.W analizowanych póbkach (o różnej granulacji cząstek osadu) wykryto i oznaczono względnie duże stężenie TBT, DBT, MBT oraz MPhT. Osady portowe...
-
Antimicrobial and surface activity of 1-alkyl-3-methylimidazolium derivatives
PublikacjaWiedza na temat zależności struktura-aktywność umożliwia projektowanie i syntezę nowych kationowych związków amfifilowych ze zoptymalizowaną aktywnością antymikrobową na rzecz przyszłego rozwoju nowych środków dezynfekujących, sanityzujących czy konserwujących. Potrzeba projektowania i identyfikowania nowych związków posiadających właściwości przeciwbakteryjne jest rezultatem pojawienia się bardziej odpornych mikroorganizmów w...
-
New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublikacjaChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
-
Indirect Measurement of Motor Current Derivatives in PMSM Sensorless Drives
PublikacjaMotor current derivatives contain useful information for control algorithms, especially in sensorless electric drives. The measurement of motor current derivatives in electric motors supplied by voltage source inverter can be performed using di/dt transducers. However, in such a solution additional sensors have to be installed, e.g. Rogowski coils. Another approach is to measure current derivatives indirectly – by oversampling...
-
Fractional Problems with Right-Handed Riemann-Liouville Fractional Derivatives
PublikacjaIn this paper, we investigate the existence of solutions for advanced fractional differential equations containing the right-handed Riemann-Liouville fractional derivative both with nonlinear boundary conditions and also with initial conditions given at the end point T of interval [0,T ]. We use both the method of successive approximations, the Banach fixed point theorem and the monotone iterative technique, as well. Linear problems...
-
Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
-
Therapeutic Potential of Carnosine and Its Derivatives in the Treatment of Human Diseases
PublikacjaDespite significant progress in the pathogenesis, diagnosis, treatment, and prevention of cancer and neurodegenerative diseases, their occurrence and mortality are still high around theworld. The resistance of cancer cells to the drugs remains a significant problem in oncology today,while in the case of neuro-degenerative diseases, therapies reversing the process are still yet to be found. Furthermore, it is important to seek new...
-
Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublikacjaMycophenolic 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...
-
Expedited antenna optimization with numerical derivatives and gradient change tracking
PublikacjaDesign automation has been playing an increasing role in the development of novel antenna structures for various applications. One of its aspects is electromagnetic (EM)-driven design closure, typically applied upon establishing the antenna topology, and aiming at adjustment of geometry parameters to boost the performance figures as much as possible. Parametric optimization is often realized using local methods given usually reasonable...
-
NUMERICAL ESTIMATION OF HULL HYDRODYNAMIC DERIVATIVES IN SHIP MANOUVERING PREDICTION
PublikacjaOperating in crowded waterways pose a risk of accidents and disasters due to maneuvering limitations of the ship. In order to predict ship’s maneuvering characteristics at the design stage, model tests are often executed as the most accurate prediction tool. Two approaches can be distinguished here: free running model tests and numerical simulations based on planar motion model with the use of hydrodynamic derivatives obtained...
-
Numerical Estimation of Hull Hydrodynamic Derivatives in Ship Maneuvering Prediction
PublikacjaPrediction of the maneuvering characteristics of the ship at the design stage can be done by means of model tests, computational simulations or a combination of both. The model tests can be realized as direct simulation of the standard maneuvers with the free running model, which gives the most accurate results, but is also the least affordable as it requires very large tank or natural lake, as well as complex equipment of the...
-
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...
-
Antifungal action of the oxathiolone-fused chalcone derivative
PublikacjaAMG-148, pochodna chalkonu z pierścieniem oksatiolonowym, wykazuje aktywność przeciwgrzybową in vitro wobec szczepów grzybowych patogennych dla człowieka, z wartościami minimalnych stężeń hamujących wzrost mieszczących się w zakresie 1-16 mikrogramów na mililitr, natomiast w wyższych stężeniach związek ten działa grzybobójczo. Obecność głównych białek oporności wielolekowej, Cdr1p, Cgr2p lub Mdr1p nie wpływa znacząco na aktywność...
-
Reduction of Derivative pipeline effort in water turbine
PublikacjaThe paper presents an approach to evaluate and reduce the effort of the derivative pipeline in a water turbine of a hydrostatic power station in its vulnerable spots. Potential places of the biggest effort of the structure, as well as the coefficient of displacement and safety factor related to them were identified using FEM numerical method. Pipeline reinforcement was designed and made based on FEM analysis. Original technology...
-
Efficient synthesis and antifungal investigation of nucleosides’ quaternary ammonium salt derivatives
PublikacjaQuaternary ammonium salts are a group of compounds with diverse biological properties, the most important of which are their antiviral, antibacterial, and antifungal activities. The quaternization reactions of 5'-O-tosyl derivatives of uridine and thymidine with triethylamine, trimethylamine, 4-(N ,N -dimethylamino)pyridine, 2-methylpyridine, and pyridine are described in this article. Two of the synthesized compounds are exceptional...
-
Fully scalable one-pot method for the production of phosphonic graphene derivatives
PublikacjaGraphene oxide was functionalized with simultaneous reduction to produce phosphonated reduced graphene oxide in a novel, fully scalable, one-pot method. The phosphonic derivative of graphene was obtained through the reaction of graphene oxide with phosphorus trichloride in water. The newly synthesized reduced graphene oxide derivative was fully characterized by using spectroscopic methods along with thermal analysis. The morphology...
-
Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
-
Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublikacjaThe 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...
-
Synthesisand cytotoxic activity of conjugates of muramyl and normuramyl dipeptides with batracylin derivatives
PublikacjaOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej batracyliną i pochodnymi batracyliny. Opracowano udoskonaloną metodę syntezy batracyliny. Zaproponowana metoda pozwala na otrzymanie BAT w skali multi-gramowej. Zsyntetyzowane analogi nie wykazały aktywności cytotoksycznej w badaniach prowadzonych w NCI (Bethesda, USA). W testach in vitro przeprowadzonych w Akademii Medycznej w Gdańsku dwa analogi redukowały...
-
Synthesis and antitumor activity of conjugates of muramyldipeptide or normuramyldipeptide with hydroxyacridine/acridone derivatives
PublikacjaOpisano syntezę analogów MDP oraz nor-MDP modyfikowanych w części peptydowej pochodnymi hydroksyakrydyny/akrydonu i dwóch analogów modyfikowanych pochodnymi 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny. Tylko związki zawierające pochodne 1-nitro-9-hydroksyetylo(propylo)aminoakrydyny wykazały wysoką aktywność cytotoksyczną badaną na 60 liniach ludzkich komórek nowotworowych, na nowotwór prostaty i AIDS-related lymphoma (ARL). Związek...
-
New class of quaternary ammonium salts, derivatives of methyl D-glucopyranosides.
PublikacjaReakcja zasad azotowych z 6-O-p-tozylo-alfa-D-glukopiranozydem metylu lub 6-O-tozylo-beta-D-glukopiranozydem metylu (prowadzona w skali mikro) dając odpowiednie sole amoniowe. Jako zasady azotowe użyto pirydyny, 2-metylopirydyny i trimetyloaminy. Produkty zostały przebadane przy użyciu spektroskopii 1H, 13C NMR, spektroskopii mas oraz analizy elementarnej a budowa jednego z nich została dodatkowo potwierdzona za pomocą rentgenowskiej...
-
Studies of the effects of antifungal cationic derivatives of amphotericin B on human erythrocytes.
PublikacjaBadano nową grupę kationowych pochodnych amfoterycyny B pod kątem zależności pomiędzy ich zdolnością do asocjacji i selektywną toksycznością. We wszystkich przypadkach stosowano amfoterycynę B jako związek odniesienia. Jako miarę efektu toksycznego in vitro badanych związków stosowano wypływ wewnątrzkomórkowego potasu oraz hemolizę. Miarą aktywności przeciwgrzybowej był MIC i utrata potasu wewnatrzkomórkowego. Do oceny stopnia...