Wyniki wyszukiwania dla: SULFONAMIDE DERIVATIVES
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Complexation of amino acids derivatives in water by calix[4]arene phosphonic acids
PublikacjaSeries of the calix[4]arene phosphonic acids with various substituents at the lower rim was synthesized. Complexing properties of these receptors towards methyl esters of six amino acids strongly depended on the calix[4]arene conformation flexibility. The complex formation processes were monitored using 1H NMR spectroscopy (deuterated phosphate buffer at pD 7.3, 22 oC) and association constant values were evaluated. Inherently...
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Comparative evaluation of new dihydropyrimidine and dihydropyridine derivatives perturbing mitotic spindle formation
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NK1 receptor binding of a few low molecular weight 3,5-bistrifluoromethylbenzene derivatives
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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The Chemometric Evaluation of Antitumor Activity of Novel Benzensulfonamide Derivatives Based on their Physiochemical Properties
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QSAR Analysis of Selected Antimicrobial Structures Belonging to Nitro-derivatives of Heterocyclic Compounds
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Influence of cellulose fibers on physicochemical properties of biodegradable films based on polysaccharide derivatives
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New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
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Interaction of amphotericin B and its selected derivatives with membranes: molecular modeling studies
PublikacjaJest to praca przeglądowa obejmująca krytyczną analizę danych dotyczących oddziaływania amfoterycyny B (AmB) i jej wybranych, mniej toksycznych pochodnych, z błonami lipidowymi. Amfoterycyna B jest antybiotykiem przeciwgrzybowym ale ze względu na jej toksyczność trwają prace nad modyfikacjami chemicznymi tego związku. Celem molekularnym dla tego antybiotyku jest błona lipidowa i dlatego różnicowe powinowactwo AmB i jej pochodnych...
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Synthesis and biological evaluation of thiophosphate tricyclic coumarin derivatives as steroid sulfatase inhibitors
PublikacjaSteroid sulfatase (STS) enzyme inhibition is an important approach to the management of hormone-dependent breast cancer. In this paper, we report convenient methods for the synthesis and biological evaluation of thiophosphate tricyclic coumarin analogs exhibiting STS activity. The described methods are based on the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-2-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one,...
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Comparison of the ability to induce apoptosis by acridine derivatives in solid tumor and leukemia cells
PublikacjaW pracy wykazano różną wrażliwość komórek nowotworowych do ulegania apoptozie pod wpływem pochodnych akrydyny.
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Efficient synthesis of N-benzyloxycarbonyl- and N-tert-butoxycarbonyl-(S)-isoserine and their derivatives
PublikacjaOpisano wydajną metodę syntezy N-benzyloksykarbonylo- i N-tert-butoksykarbo-nylo-(S)-izoseryny i jej pochodnych z kwasu L-jabłkowego poprzez odpowiednie oksazolidinony i hydrolizę tych połączeń za pomocą wodorotlenku benzylowo-trimetyloamoniowego.
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Synthesis and application of tetrazole di and triamide derivatives in ion-selective membrane electrodes
PublikacjaA number of tetrazole diamides and triamides have been synthesized and applied as ion carries in ion-selective membrane electrodes. Their selectivity and sensitivity were studied towards alkali, alkaline earth, transition and heavy metal cations. it was found that membranes doped with 3 and 2-nitrophenyl octyl ether exhibit an almost theoretial Nernstian response for NH+ over relatively wide concentration range. Elestrodes with...
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Synthesis, spectroscopy and computational studies of some novelphosphorylated derivatives of quinoline-5,8-diones
PublikacjaThe neutral phosphorus nucleophiles such as R2P(=Y)M allowed the radical addition to 2-methyl-5,8-dioxo-5,8-dihydroquinoline-7-amine and N-(2-methyl-5,8-dioxo-5,8-dihydroquinolin-7-yl)acetamide giving exclusively O-phosphorylated products. All products were quantitatively prepared and characterized by microanalysis, and multinuclear NMR spectroscopy. Seven of them, have been characterized by single crystal X-ray diffraction method....
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Design and synthesis of new analogues of batracylin linked to tuftsin and retro-tuftsin derivatives
PublikacjaThe synthesis of derivatives of batracylin with several peptides was elaborated followed by their cytotoxic activity investigation.
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Developments in the synthesis and biological activity of Glycyl-L-Histydyl-L-Lysine derivatives
PublikacjaWe emphasize on the methods of the synthesis described in the literature and present the aspects of Gly-His-Lys structure modifications that played a key role in scientific research.
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Reactivity of Diimido Complexes of Molybdenum and Tungsten towards Lithium Derivatives of Diphosphanes and Triphosphanes
PublikacjaThe reaction of R2P–P(SiMe3)Li (R = tBu, iPr) with the diimido molybdenum complex [(ArN)2MoCl2·dme] (Ar = 2,6-iPr2C6H3; dme = 1,2-dimethoxyethane) yielded the side-oncoordinated phosphanylphosphinidene anionic complexes [(2,6-iPr2C6H3N)2Mo(Cl)(η2-P=PR2)]– (7Mo, 8Mo). The thermal decomposition of [(2,6-iPr2C6H3N)2M(Cl)(η2-P=PR2)]–[M = Mo (7Mo), W (8W)] to [(2,6-iPr2C6H3N)2M(Cl)(1,2-η-tBu2P=P–PtBu2)] [M = Mo (3Mo), W (3W)] was investigated...
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DFT study of low-energy electron interaction with pyridine, pyrazine and their halo derivatives
PublikacjaIn this work, the density functional theory with B3LYP hybrid functional was employed to calculate quantities useful for estimating the behavior of pyridine, pyrazine and their derivatives monosubstituted with Cl or Br atom, when exposed to low-energy electron impact. Vertical electron affinities obtained in several Pople basis sets and in aug-cc-pVTZ basis set are reported. Although some of the investigated molecules do not form...
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Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity
PublikacjaFungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast...
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Linear and Nonlinear Optical Properties of Azobenzene Derivatives Modified with an (Amino)naphthalene Moiety
PublikacjaThe design of two-photon absorbing azobenzene (AB) derivatives has received much attention; however, the two-photon absorption (2PA) properties of bis-conjugated azobenzene systems are relatively less explored. Here, we present the synthesis of six azobenzene derivatives and three bisazobenzenes substituted (or not) at para position(s) with one or two amino group(s). Their linear and nonlinear absorption properties are studied...
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Exposure scenario and risk assessment of infants and newborns to bisphenols and their derivatives from diapers
PublikacjaNewborns and infants are more sensitive to harmful compounds such as bisphenols and their derivatives because of their not fully developed detoxification mechanism. Exposure to these substances can lead to developmental problems and health consequences in adulthood. Since disposable baby diapers are used from the first days of life and remain in contact with the baby skin, it seems important to monitor the levels of endocrine disrupting chemicals...
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The effect of anthraquinone derivatives (C1-C9) 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 (C-C9) on telomerase activity was analyzed using lysates from drug-treatedcancer cell line.
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Photoresponsive, amide-based derivative of embonic acid for anion recognition
PublikacjaThe synthesis and ion-binding properties of amide-based derivative of embonic acid andp-aminoazobenzenewere described. The new compound was characterized by X-ray structural analysis and spectroscopic methods.Ligand interacts in acetonitrile with Y-shaped anions (benzoates and acetates) and dihydrogen phosphatesforming complexes of 1:1 stoichiometry. In more polar DMSO the complexes stoichiometry changes to 2:1(L:anion). Light-inducedtranstocisisomerization...
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Fractional equations of Volterra type involving a Riemann Liouville derivative
PublikacjaIn this paper, we discuss the existence of solutions of fractional equations of Volterra type with the Riemann Liouville derivative. Existence results are obtained by using a Banach fixed point theorem with weighted norms and by a monotone iterative method too. An example illustrates the results.
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On the derivative of the Legendre function of the first kind with respect to its degree
PublikacjaPokazano, że pochodna po indeksie funkcji Legendre'a pierwszego rodzaju, obliczona dla całkowitej wartości indeksu, może być wyrażona przez funkcje elementarne. Skonstruowano kilka jawnych reprezentacji tej pochodnej. Zaprezentowano przykłady zastosowań otrzymanych wzorów.
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Unexpected thioketene derivative formation during thioacyl dithiophosphate synthesis.
PublikacjaZbadano zakres i ograniczenia tioacylowania opartego na ditiofosforanach tioacylu. Ditiofosforany tioacylo otrzymano w wyniku reakcji ditiofosforanów acylu z kwasem ditiofosforowym. Obecność dwóch podstawników w pozycji alfa we fragmencie acylowym faworyzowała tworzenie pochodnych tioketenu tym samym obniżając wydajność oczekiwanych ditiofosforanów tioacylu.
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Synthesis and properties of carboxy derivative of Epidian 6 monomethacrylate (in English)
PublikacjaWe present the synthesis of an oligomer with carboxy and methacrylic groups based on Epidian 6. The effect of the catalyst nature and amount, solvent nature and process temperature on the rate of the reaction between Epidian6 monomethacrylate and adipic acid was examined at 313, 323 and 333 K in the presence of 4-dimethylaminopyridine, 1,4-diazobicyclo[2.2.2]octane, and benzyltriammonium chloride. The synthesized oligomer was characterized...
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Carboxy derivative of dioxydiphenylpropane diglycydyl ether monomethacrylate as an addtive for composites
PublikacjaThe modifier of composites was used in the presence of polyetylene polyamine. Physico-mechanical properties and chemical stability of coatings thus obtained were analyzed.
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublikacjaA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publikacja6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Thermal Decomposition of Carbamoyl Meldrum’s Acids: A Starting Point for the Preparation of 1,3-Oxazine Derivatives
PublikacjaThe ability to undergo [4 + 2] versus [2 + 2] cycloaddition was under investigation for ketenes thermally generated from carbamoyl Meldrum’s acid. Usually, 1,3-oxazino-5-carbamoylo-4,6-diones are formed when carbamoyl Meldrum’s acid reacts with imine. However, in some cases, a reaction takes an unexpected course, leading to the formation of tetraponerines alkaloids derivatives or cyclic iminoethers.
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressant
PublikacjaZaprezentowano syntezę koniugatów adenozyny z pochodnymi muramylo- i nor-muramylodipeptydów zawierających w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako substrat zastosowano rybozyd 6-chloropuryny, który łączono poprzez 1,2-diaminoetan z odpowiednimi pochodnymi MDP lub nor-MDP w obecności EDCI i HOBt. Struktury otrzymanych związków zostały potwierdzone widmami 1H i 13C NMR (500 MHz), widmami MS oraz...
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Chromane helicity rule – scope and challenges based on an ECD study of various trolox derivatives
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Effect of thienyl units in cyanoacrylic acid derivatives toward dye-sensitized solar cells
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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Structure–bioavailability relationship study of genistein derivatives with antiproliferative activity on human cancer cell
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Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells
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Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
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Two novel nucleoside ester derivatives of chlorambucil as potential antileukemic prodrugs: a preliminary study
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Synthesis and photo-conversion of androsta- and pregna-5,7-dienes to vitamin D3-like derivatives
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Solvent effects on fluorescence properties of protochlorophyll and its derivatives with various porphyrin side chains
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Chapter 22. Antimicrobial and surface activity of 1-alkyl-3-methyl imidazolium derivatives
PublikacjaCiecze jonowe wykazują aktywność przeciwgrzybową oraz przeciwbakteryjną zależną od struktury badanego związku. Zbadano wpływ długości łańcucha alkilowego w kationie na aktywność przeciwmikrobiologiczną oraz przedstawiono zależność pomiędzy tą aktywnością a krytycznym stężeniem micelizacji imidazolowych cieczy jonowych.
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Influence of a lipid bilayer on the conformational behavior of amphotericin B derivatives - A molecular dynamics study.
PublikacjaAmphotericin B (AmB) is an effective but very toxic antifungal antibiotic. In our laboratory a series of AmB derivatives of improved selectivity of action was synthesized and tested. To understand molecular basis of this improvement, comparative conformational studies of amphotericin B and its two more selectivederivatives were carried out in an aqueous solution and in a lipid membrane. These molecular simulation studies revealed...
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Relationship between electronic structure and geometry of silanethiols and their derivatives. Elucidation of copper group silanethiolates
PublikacjaWyznaczono strukturę elektronową wybranych silanotioli X3SiSH (dla X=H, C2H5, OCH3, F, Cl i Br) oraz powstalych z nich anionów. Geometrię i funkcje falowe wyznaczono przy użyciu teorii funcjonałów gęstości elektronowej DFT. Przeanalizowano wpływ efektów anomerycznych oraz wielkości calki nakładania sigma(Si-S) na obserwowane skrócenie wiązania Si-S przy deprotonowaniu silanotioli. Podano nowe wyjaśnienie wyjątkowo niskiej kwasowości...
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Synthesis of new conjugates of MDP and nor-MDP with retro-tuftsin derivatives as potential immunomodulators
PublikacjaZsyntetyzowano nowe analogi muramylodipeptydu (MDP) i nor-muramylo-dipeptydu (nor-MDP) z pochodnymi retro-tuftsyny jako potencjalne immunomodulatory. Przedstawiono także syntezę odpowiednich pochodnych retro-tuftsyny. Do syntezy wykorzystano metodę mieszanych bezwodników z chloromrówczanem izobutylu i N-metylomorfoliną w bezwodnym DMF.
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Skin cancer, including related pathways and therapy and the role of luteolin derivatives as potential therapeutics
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Pharmacological Profile and Molecular Modeling of Cyclic Opioid Analogues Incorporating Various Phenylalanine Derivatives
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The influence of different expression of CYP3A4 izoenzymes on metabolic pathway derivatives in human hepatoma cells
PublikacjaCelem przeprowadzonych badań było określenie różnic w metabolizmie pochodnych C-857 i C-1748 w komórkach ludzkiego nowotworu wątroby HepG2 oraz określenie wpływu na ich biotransformację w podwyższonej ekspresji izoenzymu CYP3A4 w tejże linii. Uzyskane wyniki wskazały, że związek C-857, jak również C-1748 metabolizuje w komórkach HepG2 oraz Hep3A4 do wielu reaktywnych, niestabilnych metabolitów. Różnice w biotransformacji były bardzo...
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An In Vitro Antimicrobial, Anticancer and Antioxidant Activity of N–[(2–Arylmethylthio)phenylsulfonyl]cinnamamide Derivatives
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