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Search results for: BISPHENOL A ANALOGS
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Glutamine analogues containing a keto function - novel inhibitors of fungal glucosamine-6-phosphate synthase
PublicationW publikacji przedstawiono syntezę nowych pochodnych kwasu (S)-2,3-diaminopropanowego, zawierających reszty kwasów z funkcją ketonową. Dla otrzymanych związków zbadano właściwości inhibicyjne w stosunku do grzybowej syntazy glukozamino-6-fosforanu, ustalono właściwości lipofilowe otrzymanych związków a także aktywność przeciwgrzybową. Dla kilku wybranych pochodnych otrzymano ich dipeptydy, zbadano także ich aktywność przeciwgrzybową...
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Synthesis, Structure, and Spectroscopic Properties of Calcium Thiophenecarboxylate Polymers. Structural Comparison with Analogous Lead Complexes
PublicationThree novel calcium coordination polymers [Ca(2tpCOO)2(2mpa)(H2O)]n (1), [Ca(3tpCOO)2(2mpa)(H2O)]n (2), and {[Ca(3tpacCOO)2(H2O)2]⋅⋅⋅H2O}n (3) (2tpCOO− or 3tpCOO− – thiophene-2- or thiophene-3-carboxylate, 3tpacCOO− – thiophene-3-acetate, 2mpa – 2-methylpropanal), were synthesised using a self-assembly method. The obtained polymers were characterised using SC-XRD, FTIR, UV-Vis DRS, thermogravimetric and luminescence analyses. The...
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Crystal structures of eight- and ten-membered cyclic bisanisylphosphonothioyl disulfanes and comparison with their P-ferrocenyl analogues
PublicationTwo new crystal structures of eight- and ten-membered cyclic bisanisylphosphonothioyl disulfanes, namely 2,5-bis(4-methoxyphenyl)-1,6,3,4,25,55- dioxadithiadiphosphocane-2,5-dithione, C16H18O4P2S4, and 2,5-bis(4-methoxyphenyl)-1,6,3,4,25,55-dioxadithiadiphosphecane-2,5-dithione, C18H22O4P2S4, have been determined and compared to structures of the ferrocenyl analogues. The eight-membered rings have similar conformations (TBC) but...
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Structural changes of water caused by non-electrolytes: Volumetric and compressibility approach for urea-like analogues
PublicationHydration of thiourea (TU), hydroxyurea (HU, hydroxycarbamide), acetone (AC, 2-propanone) and dimethyl sulfoxide (DMSO) has been investigated with the help of the volumetric and compression measurement. The apparent molar volumes and the apparent molar isentropic (adiabatic) compression have been calculated from the density and speed of sound data at temperatures ranging from 288.15 to 308.15 K at atmospheric pressure (0.1 MPa)....
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Antibiotic-sterol interactions provide insight into the selectivity of natural aromatic analogues of amphotericin B and their photoisomers
PublicationAromatic heptaene macrolides (AHMs) belong to the group of polyene macrolide antifungal antibiotics. Members of this group were the first to be used in the treatment of systemic fungal infections. Amphotericin B (AmB), a non-aromatic representative of heptaene macrolides, is of significant clinical importance in the treatment of internal mycoses. It includes the all-trans heptaene chromophore, whereas the native AHMs contain two...
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Synteza i ocena biologiczna oligopeptydowych analogów akrydyny/akrydonu jako potencjalnych leków przeciwnowotworowych
PublicationNiniejsza praca doktorska obejmuje syntezę oraz testy aktywności biologicznej nowych analogów akrydyny/akrydonu z pochodnymi tuftsyny/retro-tuftsyny jako potencjalnych leków przeciwnowotworowych. Akrydyny należą do grupy policyklicznych związków heteroaromatycznych. Ich struktura chemiczna wywodzi się z trójpierścieniowego związku aromatycznego, będącego analogiem antracenu zawierającego atom azotu w pierścieniu B. Związki te powszechnie...
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
PublicationSome inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Hence, the discovery of CB1 inverse agonists with a chemical scaffold distinct from these holds promise for developing...
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Effects of lightning and sprites on the ionospheric potential, and threshold effects on sprite initiation, obtained using an analog model of the global atmospheric electric circuit
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The application of isotopically labeled analogues for the determination of small organic compounds by GC/MS with selected ion monitoring
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Effect of resveratrol analogue, DMU-212, on antioxidant status and apoptosis-related genes in rat model of hepatocarcinogenesis
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QSAR, QSPR and QSRR in Terms of 3-D-MoRSE Descriptors for In Silico Screening of Clofibric Acid Analogues
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Natural Quercetin Analogues Modulate Oxidative Stress Tolerance and Increase Lifespan Extension of S. cerevisiae ( proceeding)
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Synthesis and biological activity of tuftsin, its analogues and conjugates containing muramyl dipeptides of nor-muramyl dipeptides
PublicationOpisano syntezę koniugatów MDP oraz nor-MDP modyfikowanych w części peptydowej tuftsyną oraz pochodną tuftsyny zawierającą grupę nitrową. Zsyntetyzowane związki zostały przebadane in vitro na ludzkich monocytach i limfocytach w Akademii Medycznej w Gdańsku. Niektóre z nich wykazały szybsze i skuteczniejsze działanie w porównaniu z tuftsyną.
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Docking simulations, Molecular properties and ADMET studies of novel Chromane6,7diol analogues as potential inhibitors of Mushroom tyrosinase
PublicationResearch on inhibition of tyrosinase enzyme has attained significant value, because tyrosinase inhibitors have potential applications in medicine, cosmetics (as whitening agents) and in agriculture (as bioinsecticides). Determination and elucidation of new tyrosinase inhibitors are not only beneficial for medical purposes, but their promising applications in improving food quality and nutritional...
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Spliced analogues of trypsin inhibitor SFTI‐1 and their application for tracing proteolysis and delivery of cargos inside the cells
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Investigation of Serine‐Proteinase‐Catalyzed Peptide Splicing in Analogues of Sunflower Trypsin Inhibitor 1 (SFTI‐1)
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A comparison of geometric analogues of holographic reduced representations, original holographic reduced representations and binary spatter codes
PublicationGeometric Analogues of Holographic Reduced Representations (GA HRR) 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 paper reports a battery of tests aimed at comparison of GA HRR with Holographic Reduced Representation (HRR) and Binary Spatter Codes (BSC). Firstly, we perform a test of...
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Peptide conjugates of lactoferricin analogues and antimicrobials—Design, chemical synthesis, evaluation of antimicrobial activity and mammalian cytotoxicity
PublicationEight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and oneof the three antimicrobials — ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) — were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the “click chemistry” method. This novel approach is reported here...
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Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes
PublicationThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase...
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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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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublicationA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Solution conformational study of Scyliorhinin I analogues with conformational constraints by two-dimensional NMR and theoretical conformational analysis
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Use of NMR and Fluorescence Spectroscopy as well as Theoretical Conformational Analysis in Conformation-activity Studies of Cyclic Enkephalin Analogues
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Interactions of vasopressin and oxytocin receptors with vasopressin analogues substituted in position 2 with 3,3′-diphenylalanine - a molecular docking study
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Micelle-bound conformations of neurohypophyseal hormone analogues modified with a Cα-disubstituted residue: NMR and molecular modelling studies
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Highly Potent Antidiuretic Antagonists: Conformational Studies of Vasopressin Analogues Modified with 1-Naphthylalanine Enantiomers at Position 2
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Molecular modelling of transition state analogue inhibitors of glucosamine-6-P synthase and glucose-6-P isomerase.
PublicationStruktura kompleksu 2-amino-2-deoksy-D-glucitolo-6-P (ADGP) z centrum aktywnym syntazy GlcN-6-P z E. coli została wykorzystAna jako punkt wyjścia do modelowania molekularnego analogów ADGP. Używając programu GROMOS96 wygenerowano konformacje analogów o najniższych energiach wewnętrznych, które następnie ''dokowano'' w centrum aktywnym enzymu. Dokonano syntezy wybranych związków i określono parametry kinetyczne i termodynamiczne...
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Peptide splicing in a double‐sequence analogue of trypsin inhibitor SFTI‐1 substituted in the P1 positions by peptoid monomers
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Electrodes consisting of PEDOT modified by Prussian Blue analogues deposited onto titania nanotubes – Their highly improved capacitance
PublicationIn this work we present the outstanding energy storage of prepared inorganic-organic heterojunction where hydrogenated ordered titania nanotubes (H-TiO2NT) were modified by the hybrid made of poly(3,4-ethylenedioxythiophene) (pEDOT) and iron hexacyanoferrate centres (Fehcf, Prussian Blue). The material TiO2NT/pEDOT:Fechf was obtained electrochemically by means of: anodization, hydrogenation and finally, electropolymerization of...
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Synteza nowych aminokwasowych i peptydowych analogów kwasu mykofenolowego oraz ich aktywność biologiczna i mikrobiologiczna
PublicationKwas mykofenolowy (MPA) oraz jego dwie stosowane klinicznie pochodne: mykofenolan sodu (MPS, CellCept) i mykofenolan mofetylu (MMF, Myfortic) są jednymi z najczęściej używanych leków hamujących proliferację limfocytów. Obok aktywności immunosupresyjnej, farmaceutyk wykazuje również właściwości przeciwbakteryjne, przeciwgrzybicze, przeciwwirusowe a także przeciwnowotworowe. W ramach realizacji swojej pracy doktorskiej zaprojektowałam...
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Development of thin film SPME sorbents based on deep eutectic solvents and their application for isolation and preconcentration of endocrine-disrupting compounds leaching from diapers to urine
PublicationIn this study, the thin film solid phase microextraction (TF-SPME) based on a novel sorbent composed of deep eutectic solvent (DES) is proposed. Among several synthesized sorbents the most efficient was DES containing trihexyl(tetradecyl)phosphonium chloride and docosanol mixed with polydimethylsiloxane (PDMS) in a molar ratio 1:3:0.25 to achieve a more stable structure. The proposed sorbent was applied on a fiberglass mesh and...
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Genotoxic effects of antitumor 1-nitroacridines C-857 and its novel analoque 4-methyl-1-nitroacridine C-1748
Publication4-podstawione 1-nitroakrydyny reprezentują nową grupę pochodnych akrydyny zsyntetyzowanych na Politechnice Gdańskiej. W przeprowadzonych badaniach nad pochodnymi C-1748 i C-857 zastosowano dwie metody badawcze: test kometowy oraz zmodyfikowany test mikrojąderkowy (CBMN assay). W teście kometowym wykazano wzrost uszkodzeń DNA w zależności od czasu i stężenia badanych pochodnych 1-nitroakrydyny. Badania aberracji chromosomalnych...
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Evaluation of Chemotherapeutic Activity of the Selected Bases’ Analogues of Nucleic Acids Supported by ab initio Various Quantum Chemical Calculations
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Raman and surface-enhanced Raman spectroscopy investigation of vasopressin analogues containing 1-aminocyclohexane-1-carboxylic acid residue
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Influence of bulky 3,3′-diphenylalanine enantiomers replacing position 2 of AVP analogues on their conformations: NMR and molecular modeling studies
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Inhibitory activity of double‐sequence analogues of trypsin inhibitor SFTI‐1 from sunflower seeds: an example of peptide splicing
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A study on the protection of methionine and the reduction of methionine sulfoxide in methionine-containing analogues of the growth-modeling factor Gly-His-Lys
PublicationThe protection of methionine and the reduction of methionine sulfoxide in methionine-containing analogues of Gly-His-Lys are described. The peptides were synthesized by a solid-phase method using the standard Fmoc procedure. Simultaneous deprotection of the peptide side chain and liberation from the resin were achieved using an appropriate TFA cocktail. The TFA cocktail was selected to minimize oxidation of the methionine residue....
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Hybrid analogues of SFTI-1 modified in P1 position by β- and γ-amino acids and N-substituted β-alanines
PublicationA series of compounds containing either non-proteinogenic beta-/gamma-amino acids or N-substituted beta-alanine residues (beta-peptoid units) in P-1 specificity position were synthesized based on the structure of sunflower trypsin inhibitor 1 (SFTI-1). The compounds were synthesized on a solid support; the N-substituted beta-alanines (beta Nhlys and beta Nhphe) were introduced into a peptidomimetic chain via a two-step approach...
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Introduction of Pro and Its Analogues in the Conserved P1 Position of Trypsin Inhibitor SFTI-1 Retains Its Inhibitory Activity
PublicationA number of monocyclic SFTI-1 analogues modified in the conserved inhibitor P1 position by Pro, its L-hydroxyproline (Hyp) derivative as well as mimetics with different ring size were synthesized by the solid-phase method. Replacement of Ser6 by Pro, Hyp, and a four-member ring, L-azetidine-2-carboxylic acid (Aze), retained trypsin or chymotrypsin inhibitory activity. The determined association equilibrium constants of these 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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Synteza i badania biologiczne nowych analogów kwasu mykofenolowego z pochodnymi adenozyny jako potencjalnych leków immunosupresyjnych
PublicationPrzedstawiona praca doktorska pt. „Synteza i badania biologiczne nowych analogów kwasu mykofenolowego z pochodnymi adenozyny jako potencjalnych leków immunosupresyjnych” poświęcona jest związkom immunosupresyjnym opartym o cząsteczkę kwasu mykofenolowego oraz pochodnych adenozyny. Z medycznego punktu widzenia, gdy długotrwała choroba lub nagły przypadek powoduje nieodwracalny uraz tkanek, komórek lub niewydolność organu i żadna...
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Algebra of ontology modules for semantic agents
PublicationW środowisku Sieci Semantycznej problem precyzyjnego manipulowania jednostkami wiedzy nabiera szczególnego znaczenia. W tej publikacji dyskutujemy możliwość zaadaptowania do tego celu elastycznego aparatu algebry relacyjnej. Na bazie dysksji szkicujemy pewną szczególną analogię pomiędzy bazami danych a bazami wiedzy i używamy tej analogii do wprowadzenia algebry modułów semantycznych.
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Dynamics of hepatitis B virus quasispecies heterogeneity in association with nucleos(t)ide analogue treatment determined by MALDI-TOF MS
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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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Synergistic catalysis of Fe3O4/CuO bimetallic catalyst derived from Prussian blue analogues for the efficient decomposition of various organic pollutants
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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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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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Combined anticancer therapy with imidazoacridinone analogue C‐1305 and paclitaxel in human lung and colon cancer xenografts—Modulation of tumour angiogenesis
PublicationThe acridanone derivative 5-dimethylaminopropylamino- 8- hydroxytriazoloacridinone (C-1305) has been described as a potent inhibitor of cancer cell growth. Its mechanism of action in in vitro conditions was attributed, among others, to its ability to bind and stabilize the microtubule network and subsequently exhibit its tumour- suppressive effects in synergy with paclitaxel (PTX). Therefore, the objective of the present study...
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Iso-Partricin, an Aromatic Analogue of Amphotericin B: How Shining Light on Old Drugs Might Help Create New Ones
PublicationPartricin is a heptaene macrolide antibiotic complex that exhibits exceptional antifungal activity, yet poor selective toxicity, in the pathogen/host system. It consists of two compounds, namely partricin A and B, and both of these molecules incorporate two cis-type bonds within their heptaenic chromophores: 28Z and 30Z. In this contribution, we have proven that partricins are susceptible to a chromophore-straightening photoisomerization...
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Diminished toxicity of C-1748, 4-methyl-9-hydroxyethylamino-1-nitroacridine, compared with its demethyl analog, C-857, corresponds to its resistance to metabolism in HepG2 cells
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