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Search results for: PHOSPHORUS TACRINE ANALOGUES
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Antimicrobial Activity of Chimera Peptides Composed of Human Neutrophil Peptide 1 (HNP-1) Truncated Analogues and Bovine Lactoferrampin
PublicationThree chimera peptides composed of bovine lactoferrampin and the analogue of truncated human neutrophil peptide 1 were synthesized by the solid-phase method. In two compounds peptide chains were connected via isopeptide bond, whereas in the third one disulfide bridge served as a linker. All three chimeras displayed significantly higher antimicrobial activity than the constituent peptides as well as their equimolar mixtures. The...
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Helicity discrimination in N,N'-dibenzoyl-1,2,3,4,7,8,9,10-octahydro-1,10-phenanthrolines and their thiono- and selenocarbonyl analogues by inclusion complexation with chiral diols
PublicationX-ray crystallographic analysis of the title compounds revealed that they assume a folded helical con- formation of an approximate C2 symmetry in the solid state. Dithioamide, diselenoamide and monoselenoamide were resolved to enantiomers by inclusion crystallization with optically active diols (TADDOLs). The absolute configuration of the guest molecules in the complexes was assigned as P. The optical activity of the resolved compounds...
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An initial assessment of correlations between host- and virus-related factors affecting analogues antiviral therapy in HBV chronically infected patients
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Arginine-, d-arginine-vasopressin, and their inverso analogues in micellar and liposomic models of cell membrane: CD, NMR, and molecular dynamics studies
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Synergistic catalysis of Fe3O4/CuO bimetallic catalyst derived from Prussian blue analogues for the efficient decomposition of various organic pollutants
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Synthesis and Fluorescent Properties of 6-(4-Biphenylyl)-3,9-dihydro-9-oxo-5H-imidazo[1,2-A]purine Analogues of Acyclovir and Ganciclovir
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Kwas mykofenolowy i jego analogi. Synteza i aktywność biologiczna = Mycophenolic acid (MPA) and its analogues. Synthesis and biological activity
PublicationW artykule opisano kwas mykofenolowy (MPA)oraz jego analogi. Kwas MPA został odkryty ponad 100 lat temu i nadal pozostaje atrakcyjnym celem badań biologicznych. Z uwagi na bardzo dużą tendencję do ulegania glukuronidyzacji in vivo, ograniczone są jego możliwości zastosowań jako potencjalnego chemoterapeutyka. Otrzymane dotychczas analogi m.in. zawierające różne cykliczne ugrupowania, monocykliczne fenole i niefenolowe analogi oraz...
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Conformational latitude – activity relationship of KPPR tetrapeptide analogues toward their ability to inhibit binding of vascular endothelial growth factor 165 to neuropilin‐1
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Anthrapyridones, a novel group of antitumour non-cross resistant anthraqui-none analogues. Synthesis and molecular basis of the cytotoxic activity towards K562/DOX cells
PublicationOpracowano syntezę nowej grupy związków z grupy antrapirydonów z odpowiednimi hydrofobowymi lub hydrofilowymi podstawnikami. Badano działanie tych związków na komórkach K562/S i K562/DOX (nadekspresja P-glikoproteiny). Stwierdzono, że zwiększenie lipofilowości zwiększa szybkość P-gp zależnego efluksu z komórki.
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Contribution of UDP-glucuronosyltransferases (UGTs) in metabolism of acridinone antitumor agents, C-1311, C-1305, and their less active structural analogues, C-1330 and C-1299
PublicationCelem prowadzonych badań było określenie roli UDP-glukuronylotransferaz, uważanych za najważniejsze enzymy detoksykujące, w metabolizmie pochodnych imidazo- i triazoloakrydonu. Wykazano, że najbardziej aktywne przeciwnowotworowo związki z obu grup, tj. C-1311 i C-1305 są transformowane do O-glukuronidów, w przeciwieństwie do ich metoksylowych analogów, odpowiednio związku C-1330 i C-1299. Analiza składu mieszanin reakcyjnych zawierających...
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Molecular Docking-Based Study of Vasopressin Analogues Modified at Positions 2 and 3 with N-Methylphenylalanine: Influence on Receptor-Bound Conformations and Interactions with Vasopressin and Oxytocin Receptors
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Preliminary evaluation of selected mineral adsorbents used to remove phosphorus from domestic wastewater = Wstępna ocena przydatności wybranych adsorbentów mineralnych do usuwania fosforu ze ścieków bytowych
PublicationFour grinded mineral materials were studied for their ability of P sorption from the aq. phosphate solns. in 24-h tests by using equations of Langmuir and Freundlich isotherms. The particular sorbents contained mainly SiO254,5% Ca) 29.6%, Fe2O3 69,4% and showed the sorption capacities 56, 159, 285 or 2.4 mg/g resp.
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Conformational Studies of [11è12(CN4)]ScyII and [15è16(CN4)]ScyII? Two Scyliorhinin II Analogues by means of 2D NMR Spectroscopy and Theoretical Methods
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublicationIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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Synthetic lipopeptides as potential topical therapeutics in wound and skin care: in vitro studies of permeation and skin cells behaviour
PublicationSeveral Gly-His-Lys analogues were obtained to investigate their antimicrobial properties. Three lipophilic analogues with the structure numbering 1b, 2b, 4b, exhibit significant effect against bacteria and were selected for in vitro evaluation of skin cells behaviour. In the present studies, an in vitro model of wound repair, proliferative cell staining, and tracking of living cells were used. Cell proliferation and cell migration,...
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Wpływ surfaktantu anionowego LAS na mobilność frakcji fosforu w osadzie czynnym w zmiennych warunkach fizyczno-chemicznych
PublicationPrzedstawiono wyniki badań wpływu anionowego surfaktantu LAS na mobilność frakcji fosforu w osadzie czynnym. Podstawową rolę w procesie uwalniania fosforu do cieczy nadosadowej w warunkach beztlenowych pełniły: frakcja związana z substancją organiczną i frakcja związana z żelazem.
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Możliwości odzysku fosforu z odcieków, osadów ściekowych i popiołów po termicznym przekształcaniu osadów ściekowych
PublicationW ostatnich latach zaobserwowano rosnącą świadomość o ograniczonych zasobach fosforu. Szacuje się, że mogą one ulec wyczerpaniu w ciągu 100 lat, przy obecnym zaawansowaniu technologii. Ponad 80% wydobywanego złoża wykorzystywane jest do produkcji nawozów sztucznych oraz w przemyśle chemicznym. Taka perspektywa zwiększa zainteresowanie recyklingiem fosforu, który może być odzyskiwany ze ścieków w fazie płynnej, z odwodnionych osadów...
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublicationIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Influence of the particle size of carbonate-siliceous rock on the efficiency of phosphorous removal from domestic wastewater
PublicationtThe aim of the study was to determine the influence of the particle size of carbonate–silica rock (opoka)used in rock filters on the efficiency of phosphorus removal from domestic wastewater. The investigationswere carried out in a laboratory using a model consisting of three vertical flow filters with carbonate–silicarock of different particle sizes (G1= 1–2 mm; G2= 2–5 mm; G3= 5–10 mm). The tested rock was subjectedto decarbonising...
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The efficiency and technological reliability of biogenic compounds removal during long-term operation of a one-stage subsurface horizontal flow constructed wetland
PublicationThe paper presents the results of a study of the efficiency and technological reliability of total nitrogen and total phosphorus removal during long term operation of a one-stage constructed wetland system with subsurface horizontal wastewater flow. The flow rate of the wastewater treatment plant was 1.2m3/d during the research period. Physical and chemical analyses of raw wastewater and treated effluent were carried out in the...
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Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases
PublicationFourteen monocyclic analogues of trypsin inhibitor SFTI-1 isolated from sunflower seeds were synthesized by the solid-phase method. The purpose of this work was to establish the role of a disulfide bridge present in inhibitor's side chains of Cys3 and Cys11 in association with serine proteinases. This cyclic fragment was replaced by the disulfide bridges formed by L-pencillamine (Pen), homo-L-cysteine (Hcy), N-sulfanylethylglycine...
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COMPUTER-AIDED DESIGN OF ORGANOPHOSPHORUS INHIBITORS OF UREASE
PublicationBased on the structure of the most potential inhibitor diamidophosphate, various novel groups of inhibitors were developed by knowledge-based design approach with covalent carbon-phosphorus or carbon-phosphorus-carbon bond to improve hydrolytic stability to inhibit the microbial ureases. Designed compounds were evaluated with 10 (LigScore1, LigScore2, PLP1, PLP2, JAIN, PMF, PMF04, LUDI_1, LUDI_2 and LUDI_3) different scoring functions...
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Analiza osadów dennych pod kątem ich właściwości nawozowych
PublicationThe analysis of bottom sediments in terms of their fertilizing properties. In paper the characterize of sediments as product to nature usage was done. Analyzed material was taken from ecological treatment system located in wastewater treatment plant in Swarzewo (Pomerania Region) about flow Q= 6000 m3/d. Measurements of dry matter and organic matter content, as well as nitrogen concentrations and phosphorus fractions: loosely...
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Simple and novel synthesis of 3-(thio)phosphoryl-β-lactams by radical cyclization
PublicationRadical cyclization of phosphono-acetenamides promoted by manganese(III) acetate leads exclusively to the formation of 3-phosphoryl-β-lactams. The thiophosphoryl analogues were also prepared using this method. In particular, the presented protocol does not require the use of noble metals, while comparable methods do.
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N-phosphonomethylglycine utilization by the psychrotolerant yeast Solicoccozyma terricola M 3.1.4.
PublicationSolicoccozymaterricolaM 3.1.4., the yeast strain isolated from soil sample from blueberry cultivation in MiedzyrzecPodlaski in Poland, is capable to split of phosphorus to nitrogen and nitrogen to carbon bonds inN-phosphono-methylglycine (PMG, glyphosate). The biodegradation process proceeds in the phosphate-independent manner. Itis the first example of a psychrotolerant yeast strain able to degrade PMGviaCeN bond cleavage accompanied...
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Experimental and theoretical solubility advantage screening of bi-component solid curcumin formulations
PublicationA comprehensive experimental and theoretical screening was performed for identification of curcumin solubilizers. Experimental data led to formulation of a non-linear QSPR model correlating molecular descriptors with measured solubilities. The majority of synthesized binary systems exhibited a moderate enhancement of curcumin solubility, which was found to be the highest in the case of curcumin cocrystallized with pyrogallol. New...
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(CsX)Cu5O2(PO4)2 (X = Cl, Br, I): A Family of Cu2+ S = 1/2 Compounds with Capped-Kagomé Networks Composed of OCu4 Units
PublicationThree new salt inclusion compounds (CsX)Cu5O2(PO4)2 (X = Cl, Br, I), phosphate analogues of the kagomé mineral averievite, are reported. Their crystal structures are composed of trigonal networks of corner-sharing OCu4 anion-centered tetrahedra, forming capped-kagomé planes, which can also be regarded as two-dimensional slices along the [111] direction of a pyrochlore lattice. Magnetization and heat capacity measurements reveal...
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Emerging anticancer activity of candidal glucoseamine-6-phosphate synthase inhibitors upon nanoparticle-mediated delivery
PublicationNumerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methoxyfumaroyl)-L-2,3- diaminopropanoic acid (FMDP) has been extensively studied in order to develop its more active analogues. Several peptide−FMDP conjugates were tested to deliver FMDP to its...
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New conjugates of tuftsin and muramyl dipeptide as stimulators of human monocytes-derived dendritic cells
PublicationMuramyl dipeptide (MDP) and tuftsin are known biologically active compound displaying a significant influence on various cell populations of innate immune response. MDP, as a fragment of bacterial cell wall, stimulates not only macrophages and monocytes, but also dendritic cells. In contrast, little is known about tuftsin influence on these cells. Therefore it seemed vital to access whether tuftsin or its derivatives conjugated...
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Geometric analogue of holographic reduced representation
PublicationHolographic reduced representations (HRRs) are distributed representations of cognitive structuresbased on superpositions of convolution-bound n-tuples. Restricting HRRs to n-tuples consisting of 1,one reinterprets the variable binding as a representation of the additive group of binary n-tupleswith addition modulo 2. Since convolutions are not defined for vectors, the HRRs cannot be directlyassociated with geometric structures....
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Pollutants removal effectiveness in hydrophyte filters with sequential vertical and horizontal flow
PublicationThe object of investigations was the constructed wetland in Wiedersberg in Saxonia in Germany supplied with domestic sewage from 145 inhabitants. The biological part was composed of sequential reed beds with vertical and horizontal flow of sewage. It in one of new solutions, because up till now configuration with vertical bed situated at front of biological part of treatment was applied.The evaluation of object performance was...
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New procedure for the examination of the degradation of volatile organonitrogen compounds during the treatment of industrial effluents
PublicationWe present a new procedure for the determination of 32 volatile organonitrogen compounds in samples of industrial effluents with a complex matrix. The procedure, based on dispersive liquid–liquid microex-traction followed by gas chromatography with nitrogen-phosphorus and mass spectrometric detection, wasoptimized and validated. Optimization of the extraction included the type of extraction and disperser sol-vent, disperser solvent...
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The quality of sewage sludge stabilized for a long time in reed basins
PublicationThe aim of the work was to determine changes of long-term sewage sludge quality stabilized in reed basins from 7-15 years. The following parameters were evaluated: dry matter and organic matter concentration, nitrogen, phosphorus, and selected heavy metal (Cd, Ni, Pb, Cr, Cu, Zn) fractions. The material for the investigations was collected from 4 reed basin systems (utilisated sewage sludge) located in conventional WWTPs in Denmark...
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Analysis of efficiency of phosphates sorption by different granulation of selected reactive material
PublicationIn the light of the need to find an effective way to remove phosphorus from wastewater, studies on the suitability of sorption materials in this process should be conducted. The aim of the study was to examine the potential benefits of using selected adsorbents to reduce orthophosphates from the model solution under steady conditions. The study was conducted on a laboratory scale using synthetic wastewater with concentration of...
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The efficiency and reliability of pollutant removal in a hybrid constructed wetland with giant miscanthus and Jerusalem artichoke in Poland
PublicationIn this paper, we analysed the pollutant removal efficiency and reliability of a vertical and horizontal flow hybrid constructed wetland (CW) planted with giant miscanthus and Jerusalem artichoke. The wastewater treatment plant, located in south-eastern Poland, treated domestic sewage at an average flow rate of 1.2m3·d−1. The tests were carried out during. 5-years of operation of the sewage treatment plant (2011–2016). During this...
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Experiments on Preserving Pieces of Information in a Given Order in Holographic Reduced Representations and the Continuous Geometric Algebra Model
PublicationGeometric Analogues of Holographic Reduced Representations (GAc, which is the continuous version of the previously developed discrete GA model) employ role-filler binding based on geometric products.Atomic objects are real-valued vectors in n-dimensional Euclidean space and complex statements belong to a hierarchy of multivectors. The property of GAc and HRR studied here is the ability to store pieces of information in a given...
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Reactivity of Phosphanylphosphinidene Complex of Tungsten(VI) toward Phosphines: A New Method of Synthesis of catena-Polyphosphorus Ligands
PublicationThe reactivity of an anionic phosphanylphosphinidene complex of tungsten(VI), [(2,6-i-Pr2C6H3N)2(Cl)- W(η2-t-Bu2P=P)]Li·3DME toward PMe3, halogenophosphines, and iodine was investigated. Reaction of the starting complex with Me3P led to formation of a new neutral phosphanylphosphinidene complex, [( 2,6-i-Pr2C6H3N)2(Me3P)W(η2-t-Bu2P=P)]. Reactions with halogenophosphines yielded new catena-phosphorus complexes. From reaction with...
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Unexpected Z/E isomerism of N-methyl-O-phosphothioyl benzohydroxamic acids, their oxyphilic reactivity and inertness to amines
PublicationThiophosphinoylation of N-methyl p-substituted benzohydroxamic acids using disulfanes (method A) or diphenylphosphinothioyl chloride (method B) provides only one conformer of the respective O-phosphothioyl derivative (Xray and NMR analysis). Undergoing the P-transamidoxylation reaction is an evidence of the reversibility of thiophosphinoylation. Only those products containing strong EWG substituents in the aroyl residue or bulky...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublicationIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Charakterystyka odcieków powstających w aspekcie wyboru metody ich oczyszcania
PublicationArtykuł obejmuje analizę odcieków generowanych w zakładach utylizacji odpadów w aspekcie ich ilości i jakości oraz możliwości oczyszczania/zagospodarowania, ze szczególnym zwróceniem uwagi na metody biologiczne, najbardziej przyjaznej środowisku. Ponad trzyletnie badania prowadzono na dwóch obiektach zlokalizowanych w woj. pomorskim, gdzie pobierano próbki ścieków technologicznych, powstających podczas sortownia oraz kompostownia odpadów...
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Wstępna ocena wielkości stężeń związków azotu i fosforu odprowadzanych z wodami powierzchniowymi do Zatoki Puckiej z terenu gminy Puck
PublicationThe ferilizers used in agriculture negatively affect the surface and groundwater quality. The Bay of Puck is a semi-closed part of the Gulf of Gdańsk, which is particularly vulnerable to eutrophication caused by the inflow of nutrient substances. The Bay is surrounded by the lands intensively used in agriculture. Also a number of touristic resorts is located on its coast. The streams and rivers carry the load of nitrogen and phosphorus...
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Electrochemical Stability of Few-Layered Phosphorene Flakes on Boron-Doped Diamond: A Wide Potential Range of Studies in Aqueous Solutions
PublicationTwo-dimensional phosphorene has attracted great interest since its discovery as a result of its extraordinary properties. Two-dimensional single crystals of phosphorene can be useful for electrochemical (EC) sensing applications due to their enhanced surface-to-volume ratio. We proposed to investigate the electrochemical performance of phosphorene deposited directly on boron-doped diamond (BDD) electrodes. Noncovalent interaction...
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Ring Opening of Triflates Derived from Benzophospholan-3-one Oxides by Aryl Grignard Reagents as a Route to 2‑Ethynylphenyl(diaryl)phosphine Oxides
PublicationA new simple method for the synthesis of 2-ethynylphenyl(diaryl)phosphine oxides via ring opening of benzophosphol-3-yl triflates has been developed. This process occurs via nucleophilic attack of a Grignard reagent at the phosphorus center, which results in ring opening and cleavage of a leaving group. The reaction proceeds under mild conditions and, within 15−60 min, leads to a library of previously unavailable 2-ethynylphenylphosphine...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublicationMany people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. Todate, many acridine/acridone analogues have been obtained,which, inter alia, exhibit...
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Assessing ecotoxicity and the endocrine potential of selected phthalates, BADGE and BFDGE derivatives in relation to environmentally detectable levels
PublicationThere is no doubt that the subject area of plasticmaterials (e.g., production of epoxy resins or polyesters) is inherently connected to issues concerning bisphenol A (BPA) and its analogues. Unfortunately, much less attention has been given to other compounds, which are also used for the production of these materials. Bisphenol A diglycidyl ether (BADGE) is a synthetic industrial compound obtained by a condensation reaction between...
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Nitrification, denitrification, and dephosphatation capability of activated sludge during co-treatment of intermediate-age landfill leachates with municipal wastewater
PublicationThis study focuses on the possible use and efficacy of the co-treatment of landfill leachate (intermediate-age) with municipal wastewater. The nitrification, denitrification, and dephosphatation capability of activated sludge acclimated with a mixture of raw municipal wastewater (RWW) with gradually increasing amounts of raw landfill leachate (RLL) (from 0.5 to 5% v/v) were tested. Biochemical tests were conducted simultaneously...
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Nowe substancje psychoaktywne. Cz. I. Współczesna sytuacja narkotykowa
PublicationGwałtowny wzrost liczby substancji wprowadzanych na rynek narkotykowy został zaobserwowany już pod koniec lat dziewięćdziesiątych XX wieku. Każdego roku syntezowane są nowe substancje jako analogi już istniejących, a ich ilość systematycznie rośnie. Niejednokrotnie wprowadzenie niewielkiej zmiany w strukturze związku może spowodować znaczne zmiany ich właściwości fizykochemicznych oraz psychoaktywnych. Nowe substancje psychoaktywne...
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Fully scalable one-pot method for the production of phosphonic graphene derivatives
PublicationGraphene 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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Nowe monomery pochodzenia roślinnego w syntezie termoplastycznych elastomerów poliuretanowych
PublicationJak dotychczas w syntezie termoplastycznych elastomerów poliuretanowych (TPU) są powszechnie wykorzystywane surowce pochodzenia petrochemicznego. Sytuacja jednak zmienia się dynamicznie i w wielu gospodarkach świata widoczne są już trendy, polegające na coraz większym wykorzystaniu substancji pochodzenia roślinnego w produkcji surowców, np. glikoli, izocyjanianów czy polioli, jako zamienników analogów syntetycznych. Praca obejmuje...
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Synthesis and Properties of Di-isopropylamino Derivatives of Diphosphanes and Triphosphanes: The X-Ray Structure of (iPr2N)2P-P(SiMe3)2
PublicationPrzeprowadzono reakcję (iPr2N)2PCl z P(SiMe3)2Li w wyniku której otrzymano difosfan (iPr2N)2P-P(SiMe3)2. Strukturę związku określono przy pomocy rentgenowskiej analizy strukturalnej. Otrzymano także pochodną litową (iPr2N)2P-P(SiMe3)Li w rekcji z nBuLi. W reakcji (iPr2N)2PCl z (iPr2N)2P-P(SiMe3)Li otrzymano trifosfan (iPr2N)2P-P(SiMe3)-P(NiPr2)2 z dużą wydajnością. Próby otrzymania pochodnej litowej (iPr2N)2P-PLi-P(NiPr2)2 zakończyły...