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Search results for: MIC, ANTIMICROBIAL ACTIVITY, MURAMYL DIPEPTIDE DERIVATIVES, ANALOGUES OF ANTHRAQUINONES, RETRO-TUFTSIN DERIVATIVES
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Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
PublicationPyrazine and its derivatives are a large group of compounds that exhibit broad biological activity, the changes of which can be easily detected by a substituent effect or a change in the functional group. The present studies combined theoretical research with the density functional theory (DFT) approach (B3LYP/6-311+G**) and experimental (potentiometric and spectrophotometric) analysis for a thorough understanding of the structure...
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A five-year retrospective study shows increasing rates of antimicrobial drug resistance in Cabo Verde for both Staphylococcus aureus and Escherichia coli
PublicationObjectives Data on baseline drug resistance is important in informing future antimicrobial stewardship programs. So far, no data on the antimicrobial drug resistance of clinical isolates was available for the African archipelago of Cabo Verde. Methods We have performed a retrospective analysis over five-years (2013-17) of the antimicrombial drug susceptibility profiles of clinical isolates in the two main hospitals of Cabo Verde....
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Biopolymers in designing modern antimicrobial medical materials. Part I. Biopolymer medical materials - collagen, chitosan
PublicationThe article is a review of the literature concerning the possible use of biopolymers for the preparation of dressings with antimicrobial activity. Authors show the potential of biopolymers: collagen and chitosan - which have the ability to immobilize and control the release of various active compounds - for providing the appropriate antibacterial, bacteriostatic and wound healing properties. Types of threats, for which the dressing...
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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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The influence of different expression of CYP3A4 izoenzymes on metabolic pathway derivatives in human hepatoma cells
PublicationCelem 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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Synthesis, spectroscopy and crystal structure determination of heteroleptic cobalt(II) silanethiolates with pyridine derivatives
PublicationCztery nowe tri-tert-butoksysilanotiolanowe kompleksy kobaltu(II) z 3- i 4-metylopirydyną zostały zsyntetyzowane i scharakteryzowane. Monometaliczne kompleksy otrzymano w reakcji bimetalicznego kompleksu [Co(SSi(OtBu)3(NH3)]2, który posłużył jako substrat kobaltu(II). Nowe związki zostały scharakteryzowane przy użyciu rentgenografii strukturalnej oraz spektroskopii UV-vis i FT-IR, a także za pomocą analizy elementarnej. Kompleksy...
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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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Skin cancer, including related pathways and therapy and the role of luteolin derivatives as potential therapeutics
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Chemometric analysis of UV-Vis spektra of associated forms of Amphotericin B and its derivatives
PublicationPrzedmiotem badań był proces agregacji nowych pochodnych antybiotyku polienowego Amfoterycyny B. Do śledzenia procesu agregacji wykorzystano spektroskopię absorpcyjną w zakresie widzialnym i bliskiego nadfioletu. Zastosowanie zaawansowanych technik chemometrycznych pozwoliło na dogłębną analizę agregacji tych pochodnych, co pozwoliło na wyciągniecie następujacych wniosków: i) w przypadku wszystkich pochodnych przy stężeniach poniżej...
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Relationship between electronic structure and geometry of silanethiols and their derivatives. Elucidation of copper group silanethiolates
PublicationWyznaczono 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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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublicationBadano reakcje elektrochemicznego utleniania 2-hydroksyakrydonu, związku modelowego aktywnych przeciwnowotworowo pochodnych imidazoakrydonu. Do badań zastosowano metody woltamperometrii cyklicznej, metodę spektroelektrochemiczną oraz elektrolizę przy kontrolowanym potencjale. Badano też reakcje fotochemicznego utleniania. Badania prowadzono w ramach szerszego problemu poznania przemian aktywacji metabolicznej pochodnych hydroksyakrydonu...
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Anticancer and antimicrobial properties of novel η6-p-cymene ruthenium(ii) complexes containing a N,S-type ligand, their structural and theoretical characterization
PublicationRuthenium(II) complexes are lately of great scientific interest due to their chemotherapeutic potential asanticancer and antimicrobial agents. Here we present the synthesis of new pyrazole carbothioamidederivatives and their four arene–ruthenium complexes. The title compounds were characterized with theapplication of IR, NMR, mass spectrometry, elemental analysis and X-ray diffraction. Additionally, for newcomplexes DFT calculations...
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Synthesis, biological activity and conformational analysis of head-to-tail cyclic analogues of LL37 and histatin 5
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Glutathione conjugation of the antitumor-active 1-nitroacridine derivatives compounds C-857 and C-1748 – the major role of glutathione S-transferase M1-1
Open Research DataObjectives: C-857 and C-1748 are antitumor-active agents, monomers of unsymmetrical bisacridine derivatives. The aim of this study was to analyze their glutathione (GSH) conjugation in vitro in the presence of glutathione S-transferase (GST) M1-1.
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublicationStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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In vitro evaluation of novel lipopeptides with potential therapeutic application
PublicationThe synthesis of derivatives of Gly-His-Lys was elaborated followed by their antimicrobial activity investigation.
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Novel 5-Substituted 2-(Aylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl)benzenesulfonamides: Synthesis, Molecular Structure, Anticancer Activity, Apoptosis-Inducing Activity and Metabolic Stability
PublicationA series of novel 5-substituted 2-(arylmethylthio)-4-chloro-N-(5-aryl-1,2,4-triazin-3-yl) benzenesulfonamide derivatives 27–60 have been synthesized by the reaction of aminoguanidines with an appropriate phenylglyoxal hydrate in glacial acetic acid. A majority of the compounds showed cytotoxic activity toward the human cancer cell lines HCT-116, HeLa and MCF-7, with IC50 values below 100 M. It was found that for the analogues 36–38...
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Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublicationAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Anna Rzeczycka dr hab.
PeopleAnna Rzeczycka is the deputy head of the Department of Finance at the Faculty of Economics and Management of the Gdańsk University of Technology. Publications are situated in the field of social sciences in the discipline of economics and finance. They include books, monographs, articles, publications and scientific editions of monographs and scientific journals. In terms of numbers, it includes the following items: 12 monographs...
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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublicationOther than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach its therapeutic site of action. Despite many recent excellent achievements in the field of computational methods supporting drug metabolism studies, a well-recognized procedure to model...
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Evaluation of antimicrobial properties of thermomelt adhesives modified with zinc compounds
Open Research DataThe dataset contains the results of microbiological tests of thermomelt adhesives modified with zinc compounds, whose activity was assessed for their ability to reduce the number of Escherichia coli and Staphylococcus aureus strain, representing the Gram (-) and Gram (+) bacteria, respectively. The evaluation of antimicrobial properties of samples were...
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Antimicrobial molecular nanocarrier–drug conjugates
PublicationMany antimicrobial drugs are poorly active against pathogenic microbes causing intracellular infections, such as Mycobacterium tuberculosis or Plasmodium falciparum. On the other hand, several known antimicrobial agents are not effective enough because of their limited cellular penetration. A common feature of both challenges is the inability of an active agent to cross the biological membrane(s). One of the possible approaches...
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Chemical Aspects of Biological Activity of Isothiocyanates and Indoles, the Products of Glucosinolate Decomposition
PublicationThere is growing evidence that cancer chemoprevention employing natural, bioactive compounds may halt or at least slow down the different stages of carcinogenesis. A particularly advantageous effect is attributed to derivatives of sulfur-organic phytochemicals, such as glucosinolates (GLs) synthesized mainly in Brassicaceae plant family. GLs are hydrolysed enzymatically to bioactive isothiocyanates (ITC) and indoles, which exhibit strong...
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Amide/Amino-Based Functional Additives for Lubricants: Structure, Antimicrobial Activity and Wear Resistance
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UV Curable Coatings Based on Urethane Acrylates Containing Eugenol and Evaluation of Their Antimicrobial Activity
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Flavonoids and Essential Oil of Bidens cernua of Polish Origin and in Vitro Antimicrobial Activity of the Oil
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Lobularia libyca: Phytochemical Profiling, Antioxidant and Antimicrobial Activity Using In Vitro and In Silico Studies
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Investigation of the antimicrobial potential and microbiota of bee pollen and bee bread derived from Polish apiaries
PublicationThe phenomenon of resistance of microorganisms to antibiotics is becoming one of the greatest challenges of modern medicine. At the same time, the number of new antibiotics introduced into clinical practice is decreasing. This creates the need to search for new, effective, non-antibiotic methods of combating and preventing infectious diseases. Over the last two decades, there has been renewed interest in the antimicrobial potential...
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The assessment of microbiological antimicrobial properties of PE film loaded with nanozinc filler
Open Research DataThe dataset contains the results of a single series of determinations of the antimicrobial properties against E. coli and S. aureus of polyethylene films containing the nanozinc filler.
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Investigation of the Antifungal Activity and Mode of Action of Thymus vulgaris, Citrus limonum, Pelargonium graveolens, Cinnamomum cassia, Ocimum basilicum, and Eugenia caryophyllus Essential Oils
PublicationThe antimicrobial activity of plant oils and extracts has been recognized for many years. In this study the activity of Thymus vulgaris, Citrus limonum, Pelargonium graveolens, Cinnamomum cassia, Ocimumbasilicum, and Eugenia caryophyllus essential oils (EOs) distributed by Pollena Aroma (Nowy Dwór Mazowiecki, Poland) was investigated against a group of 183 clinical isolates of C. albicans and 76 isolates of C. glabrata. All of...
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Stabilities of bisphenol A diglycidyl ether, bisphenol F diglycidyl ether, and their derivatives under controlled conditions analyzed using liquid chromatography coupled with tandem mass spectrometry
PublicationBisphenol A diglycidyl ether (BADGE), bisphenol F diglycydyl ether (BFDGE), and their related compounds are widely used as precursors in production of epoxy resins. The high reactivity of these compounds makes the development of analytical methodologies that ensure appropriate metrological accuracy crucial. Consequently, we aimed to determine whether and to what extent the composition of the solution and storage conditions affect...
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Probiotics and Antimicrobial Proteins
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Antimicrobial resistance of fecal indicators in disinfected wastewater
PublicationThe main objective of the study was to assess the potential of three systems (UV irradiation, ozonation, and micro/ultrafiltration) operated in a pilot scale in removal of antimicrobial-resistant fecal bacteria from secondary effluent of the local wastewater treatment plant (700,000 population equivalent). The effectiveness of the processes was analysed using the removal ratio of fecal indicators (Escherichia coli and Enterococcus...
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Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α1-adrenoceptor antagonistic properties
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Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties
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New chiral discotics with helical organization of the mesophase—liquid crystalline derivatives of dibenzotetraaza[14]annulene
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Molecular dynamics study on the influence of C-terminal sugar substitution on dynamics and conformation of vancomycin derivatives
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New D−π–D−π–A Systems Based on Phenothiazine Derivatives with Imidazole Structures for Photovoltaics
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Experimental and theoretical studies of spectroscopic properties of simple symmetrically substituted diphenylbuta-1,3-diyne derivatives
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Determining the true content of quercetin and its derivatives in plants employing SSDM and LC–MS analysis
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The oxydiacetate and iminodiacetate complexes of oxidovanadium(IV) as the new series of the catalysts for the oligomerization of beta-olefin derivatives
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The new esters derivatives of betulin and betulinic acid in epidermoid squamous carcinoma treatment – In vitro studies
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Genetic and lifestyle variables associated with homocysteine concentrations and the distribution of folate derivatives in healthy premenopausal women
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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublicationN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...