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Wyniki wyszukiwania dla: ACRIDINONE DERIVATIVES
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Antimicrobial activity of 5-arylidene aromatic derivatives of hydantoin. Part 2
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Kinetics of Flavoenzyme-Catalyzed Reduction of Tirapazamine Derivatives: Implications for Their Prooxidant Cytotoxicity
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Determination of the Stereostructure of Pyrimidine Nucleoside Derivatives with a Combination of Various Chiroptical Methods
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Anti-Helicobacter pylori activity of some newly synthesized derivatives of xanthone
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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...
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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...
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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...
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N-alkyl derivatives of 2-amino-2-deoxy-D-glucose
PublikacjaMono- i di-N-alkilowe pochodne 1,3,4,6-tetra-O-acetylo-2-amino-2-deoksy-beta-D-glukozy (alkil = metyl, etyl, propyl, butyl, pentyl, heksyl, benzyl) otrzymano w wyniku redukcyjnej alkilacji per-O-acetylo-D-glukozaminy. (N-etylo, N-propylo, N-butylo, N-pentylo, N-heksylo)-1,3,4,6-tetra-O-acetylo-2-amino-2-deoksy-beta-D-glukozy deacetylowano w celu podjęcia prób enzymatycznej fosforylacji. Wszystkie produkty scharakteryzowano za pomocą...
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Synthesis of conjugates of amino-combretastatin with tuftsin derivatives as potential anticancer agents
PublikacjaOpisano syntezę nowych koniugatów 3'-N-(tuftsyno lub retro-tuftsyno)-amino-kombretastatyny jako potencjalnych związków przeciw-nowotworowych. Do syntezy amino-kombretastatyny (amino-CA-4) wykorzystano reakację Wittiga a koniugatów metodę DPPA. Mamy nadzieję, że połączenie pochodnych tuftsyny z amino-CA-4 wpłynie na polepszenie właściwości terapeutycznych CA-4.
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublikacjaA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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IPMSM rotor position estimator based on analysis of phase current derivatives
PublikacjaThis paper describes an algorithm for estimation of IPMSM angular rotor position. The algorithm uses derivatives of motor phase currents resulting from PWM modulation to obtain the rotor position. The presented method is designed for medium- and high-speed range, since it is based on determination of the EMF vector. Algorithm is characterised by a very simple formulae. The calculation of rotor position is performed in every PWM...
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Fentanyl and its derivatives as a group of new psychoactive substances (designer drugs)
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Chemosensitization of multidrug resistant Candida albicans by the oxathiolone fused chalcone derivatives
PublikacjaThree structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C.albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and derivative 18 partially reversed fluconazole...
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Macrocyclic derivatives of imidazole as chromoionophores for bismuth(III)/lead(II) pair
Publikacja18-membered diazomacrocycles with imidazole or 4-methylimidazole residue as a part of macrocycle were used as chromoionophores in bismuth(III) and lead(II) dual selective optodes for the first time. Cellulose triacetate membranes doped with macrocyclic chromoionophores are bismuth(III) and lead(II) selective with color change from orange/red to different shades of blue and violet, respectively. Results obtained for model and real...
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Azomacrocyclic derivatives of imidazole: synthesis, structure, and metal ion complexation properties
PublikacjaOtrzymano nowe azokorony zawierające resztę imidazolu w makropierścieniu. Na drodze sprzęgania z solami diazoniowymiotrzymano pochodne imidazolu 2-metylo, 4-metylo oraz 4-fenyloimidazolu. Synteza była prowadzona w warunkach wysokiego ciśnienia. Dla 21-członowej pochodnej 4-metyloimidazolu określono strukturę jej adduktu z wodą przy pomocy metod rentgenograficznych.Zdolność kompleksowania jonów metali badano spektrofotometrycznie...
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Interactions of amphotericin B derivatives with lipid membranes - a molecular dynamics study
PublikacjaW pracy analizowano oddziaływanie dwóch nisko-toksycznych pochodnych amfoterycyny B (związki SAmE i PAmE) z modelami błon lipidowych. Badania wykonane zostały za pomocą dynamiki molekularnej. Modele błon oprócz fosfolipidów DMPC zawierały odpowiednio cholesterol (model błony zwierzęcej) lub ertosterol (model błony grzybowej). Analiza wyników wykazała, że obie pochodne amfoterycyny B zachowują się inaczej w błonie cholesterolowej...
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Synthesis of conjugates of Combretastatin A-4 with tuftsin derivatives as potential anticancer agents
PublikacjaZaprezentowano syntezę nowych koniugatów Combretastatyny A-4 z pochodnymi tuftsyny i retro-tuftsyny, jako potencjalnych związków przeciwnowotworowych.
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Reaction of thio and seleno phosphoric acid derivatives with O-thioacylated hydroxylamine
PublikacjaZbadano reakcję siarkowych i selenowych analogów kwasu O,O-neopentylidenofosforowego z O-tiopiwaloilo-N-tert-butylohydroksyloaminą, w której to następuje rozszczepienie wiązania N-O. Znaleziono korelację pomiędzy potencjałem utleniającym anionu pochodnej kwasu fosforowego a przebiegiem badanej reakcji.
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Spectroscopic insight into supramolecular assemblies of boric acid derivatives and β-cyclodextrin
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Effect of renal replacement therapy on selected arachidonic acid derivatives concentration
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Solvent extraction of copper ions by 3-substituted derivatives of β-diketones
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Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives
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Artificial Neural Networks for Prediction of Antibacterial Activity in Series of Imidazole Derivatives
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In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...
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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...
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Diaryl Sulfide Derivatives as Potential Iron Corrosion Inhibitors: A Computational Study
PublikacjaThe present work aimed to assess six diaryl sulfide derivatives as potential corrosion inhibitors. These derivatives were compared with dapsone (4,4′-diaminodiphenyl sulfone), a common leprosy antibiotic that has been shown to resist the corrosion of mild steel in acidic media with a corrosion efficiency exceeding 90%. Since all the studied compounds possess a common molecular backbone (diphenyl sulfide), dapsone was taken as the...
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Reactivity of triphosphinoboranes towards H3B·SMe2: access to derivatives of boraphosphacycloalkanes with diverse substituents
PublikacjaTriphosphinoboranes activated the B–H bond in the BH3 molecule without any catalysts at room temperature. Hydroboration reactions led to boraphosphacyloalkanes with diverse structures. The outcomes of reactions depend on the size of the phosphanyl substituent on the boron atom of the parent triphosphinoborane, where derivatives of boraphosphacyclobutane and boraphosphacyclohexane were obtained. Furthermore, the precursor of triphosphinoboranes,...
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Photoelectron spectroscopy of brominated derivative of pyrimidine: 2-bromopyrimidine
PublikacjaIn this study the brominated derivative of pyrimidine, 2-bromopyrimidine, was investigated by photoelectron spectroscopy. Outer valence photoelectron spectra recorded at 21.22, 45 and 100 eV photon energy for this compound are presented. The recorded spectra have a higher resolution than that previously reported in the literature. The bromine 3d and 3p edge photoelectron spectra have also been recorded in a photon impact experiment...
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9-(2,6-dichlorophenoxycarbonyl)10-methylacridinium trifluoromethanesulfonate and its precursor 2,6-dichlorophenyl acridine-9-carboxylate
PublikacjaMetodą rentgenowskiej analizy strukturalnej oznaczono struktury obu tytułowych związków. W ich trójskośnych kryształach występują odpowiednio: układy oddziaływań elektrostatycznych, C-H...O i π-π lub C-H...Cl, π-π i oddziaływań dyspersyjnych.
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The ability to overcome multidrug resistance of tumor cell lines by novel acridine cytostatics with condensed heterocyclic rings
PublikacjaZbadano aktywność cytotoksyczną, in vitzo dwóch nowych grup cytostatyków akrydynowych zawierających skondensowane pierścienie heterocykliczne w stosunku do komórek nowotworowych linii wrażliwych i opornych. Otrzymane wyniki potwierdziły naszą wcześniejszą hipotezę o istotnej roli pierścieni hetero-cyklicznych w pokonywaniu krzyżowej oporności wielolekowej.
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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 of Usnic Acid Derivatives and Evaluation of Their Antiproliferative Activity against Cancer Cells
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Activity of isavuconazole and other triazole derivatives against clinical isolates of Aspergillus fumigatus
PublikacjaAspergillus fumigatus is the most frequent pathogen of the genus Asperillus, which is highly susceptible to triazole derivatives, especially to isavuconazole and voriconazole. Many countries face a growing problem of infections due to A. fumigatus showing acquired resistance to one or several triazoles. In medical centres, monitoring the susceptibility of isolated Aspergillus spp. is recommended. The aim of this study was to collect...
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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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Simplifying biochemical tumorous bone remodeling models through variable order derivatives
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The lipophilicity estimation of 5-arylidene derivatives of (2-thio)hydantoin with antimycobacterial activity
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Imidazo-thiazine, -diazinone and -diazepinone derivatives. Synthesis, structure and benzodiazepine receptor binding
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The Oxolane Ring Opening of Some Muramic Acid Derivatives Under Acidic Conditions
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New Benzo[h]quinolin-10-ol Derivatives as Co-sensitizers for DSSCs
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9,9′-bifluorenylidene derivatives as novel hole-transporting materials for potential photovoltaic applications
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Effect of heterocycle donor in 2-cyanoacrylic acid conjugated derivatives for DSSC applications
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Vitamin D derivatives enhance cytotoxic effects of H2O2 or cisplatin on human keratinocytes
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Synthesis and antimicrobial and nitric oxide synthase inhibitory activities of novel isothiourea derivatives
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Experimental and theoretical studies of the spectroscopic properties of simple symmetrically substituted diphenylacetylene derivatives
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Lipidation of Temporin-1CEb Derivatives as a Tool for Activity Improvement, Pros and Cons of the Approach
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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,...