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Wyniki wyszukiwania dla: MIC, ANTIMICROBIAL ACTIVITY, MURAMYL DIPEPTIDE DERIVATIVES, ANALOGUES OF ANTHRAQUINONES, RETRO-TUFTSIN DERIVATIVES
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Experimental and theoretical studies of the spectroscopic properties of simple symmetrically substituted diphenylacetylene derivatives
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Vitamin D derivatives enhance cytotoxic effects of H2O2 or cisplatin on human keratinocytes
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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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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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The mechanism of overcoming multidrug resistance (MDR) of fungi by amphotericin B and its derivatives
PublikacjaPrzeprowadzono badania porównawcze w celu określenia aktywności i cytotoksyczności amfoterycyny B (AmB) i jej pochodnych wobec standardowego szczepu S. cerevisiae i jego transformantów zawierających geny C. albicans kodujące białka oporności wielolekowej (MDR) typu ABC i MFS. Pochodne AmB: amid 3-dimetyloaminopropylowy amfoterycyny B oraz ester metylowy N-metylo-N-D-fruktopiranozylo-amfoterycyny B wykazały efekt fungistatyczny...
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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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Influence of cellulose fibers on physicochemical properties of biodegradable films based on polysaccharide derivatives
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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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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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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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New Chalcone Derivatives Containing 2,4-Dichlorobenzenesulfonamide Moiety with Anticancer and Antioxidant Properties
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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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Investigation of poly(3,4-ethylenedioxythiophene) deposition method influence on properties of ion-selective electrodes based on bis(benzo-15-crown-5) derivatives
PublikacjaGlassy carbon electrodes modified by conductive polymers and membrane with derivatives of bis(benzo-15-crown-5) were tested as solid contact ion selective electrodes for K+ ions concentration determination. PEDOT with PSS, Cl- and ClO4- counter ions was electrochemically deposited onto glassy carbon substrates using four different electrochemical approaches (potentiostatic, galvanostatic, potentiodynamic and potentiostatic pulses)....
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New 2-[(4-Amino-6-N-substituted-1,3,5-triazin-2-yl)methylthio]-N-(imidazolidin-2-ylidene)-4-chloro-5-methylbenzenesulfonamide Derivatives, Design, Synthesis and Anticancer Evaluation
PublikacjaIn the search for new compounds with antitumor activity, new potential anticancer agents were designed as molecular hybrids containing the structures of a triazine ring and a sulfonamide fragment. Applying the synthesis in solution, a base of new sulfonamide derivatives 20–162 was obtained by the reaction of the corresponding esters 11–19 with appropriate biguanide hydrochlorides. The structures of the compounds were confirmed...
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Mass spectrometry based identification of geometric isomers during metabolic stability study of a new cytotoxic sulfonamide derivatives supported by quantitative structure-retention relationships
PublikacjaA set of 15 new sulphonamide derivatives, presenting antitumor activity have been subjected to a metabolic stability study. The results showed that besides products of biotransformation, some additional peaks occurred in chromatograms. Tandem mass spectrometry revealed the same mass and fragmentation pathway, suggesting that geometric isomerization occurred. Thus, to support this hypothesis, quantitative structure-retention relationships...
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Recent developmentsinthesynthesisand biological activityofacridine/acridoneanalogues
PublikacjaMany 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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Effect of self-assembly on antimicrobial activity of double-chain short cationic lipopeptides
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Use of magnetic nanoparticles as a drug delivery system to improve chlorhexidine antimicrobial activity
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Draft genome sequence of antimicrobial producing Paenibacillus alvei strain MP1 reveals putative novel antimicrobials
PublikacjaA Paenibacillus strain isolated in previous research exhibited antimicrobial activity against relevant human pathogens including Staphylococcus aureus and Listeria monocytogenes. In this study, the genome of the aforementioned strain, designated as MP1, was shotgun sequenced. The draft genome of strain MP1 was subject to multiple genomic analyses to taxonomically characterize it and identify the genes potentially responsible for...
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New Unsymmetrical Bisacridine Derivatives Noncovalently Attached to Quaternary Quantum Dots Improve Cancer Therapy by Enhancing Cytotoxicity toward Cancer Cells and Protecting Normal Cells
PublikacjaThe use of nanoparticles for the controlled drug delivery to cells has emerged as a good alternative to traditional systemic delivery. Quantum dots (QDs) offer potentially invaluable societal benefits such as drug targeting and in vivo biomedical imaging. In contrast, QDs may also pose risks to human health and the environment under certain conditions. Here, we demonstrated that unique combination of nanocrystals core components...
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Structure-based design and evaluation of novel N-phenyl-1H-indol-2-amine derivatives for fat mass and obesity-associated (FTO) protein inhibition
PublikacjaFat mass and obesity-associated (FTO) protein contributes to non-syndromic human obesity which refers to excessive fat accumulation in human body and results in health risk. FTO protein has become a promising target for anti-obesity medicines as there is an immense need for the rational design of potent inhibitors to treat obesity. In our study, a new scaffold N-phenyl-1H-indol-2-amine was selected as a base for FTO protein inhibitors...
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Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
PublikacjaPyrazine 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
PublikacjaObjectives 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
PublikacjaThe 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
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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Synthesis, spectroscopy and crystal structure determination of heteroleptic cobalt(II) silanethiolates with pyridine derivatives
PublikacjaCztery 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
PublikacjaPrzedmiotem 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
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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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublikacjaBadano 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
PublikacjaRuthenium(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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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures 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
PublikacjaThe 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
PublikacjaA 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
PublikacjaAnthraquinones 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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Prediction of Overall In Vitro Microsomal Stability of Drug Candidates Based on Molecular Modeling and Support Vector Machines. Case Study of Novel Arylpiperazines Derivatives
PublikacjaOther 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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Antimicrobial molecular nanocarrier–drug conjugates
PublikacjaMany 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
PublikacjaThere 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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