Wyniki wyszukiwania dla: BIS-PHOSPHONIC ACID DERIVATIVES, ONE-POT SYNTHESIS
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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,...
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Photoresponsive Amide-Based Derivatives of Azobenzene-4,4′-Dicarboxylic Acid—Experimental and Theoretical Studies
PublikacjaAzobenzene derivatives are one of the most important molecular switches for biological and material science applications. Although these systems represent a well-known group of compounds, there remains a need to identify the factors influencing their photochemical properties in order to design azobenzene-based technologies in a rational way. In this contribution, we describe the synthesis and characterization of two novel amides...
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Novel Azocoumarin Derivatives—Synthesis and Characterization
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The comparison of antioxidant properties and nutrigenomic redox-related activities of vitamin C, C-vitamers, and other common ascorbic acid derivatives
PublikacjaThe term ‘vitamin C’ describes a group of compounds with antiscorbutic activity of L-ascorbic acid (AA). Despite AA’s omnipresence in plant-derived foods, its derivatives have also been successfully implemented in the food industry as antioxidants, including the D-isomers, which lack vitamin C activity. This study aimed to determine the relationship between redox-related activities for five derivatives of AA using electrochemical,...
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Synthesis and characterization of cycloaliphatic hydrophilic polyurethanes, modified with l-ascorbic acid, as materials for soft tissue regeneration
PublikacjaIn this paper we described synthesis and characteristic of obtained hydrophilic polyurethanes (PURs) modified with ascorbic acid (commonly known as vitamin C). Such materials may find an application in the biomedical field, for example in the regenerative medicine of soft tissues, according to ascorbic acid wide influence on tissue regeneration Flora (2009), Szymańska-Pasternak et al. (2011), Taikarimi and Ibrahim (2011), Myrvik...
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Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation
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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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Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking
PublikacjaHerein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process. Good quality crystals obtained for all of the synthesized compounds allowed the analysis of their molecular structures. Subsequently, the determined crystal structures were used to calculate...
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Chromogenic macrocyclic derivatives of azoles - synthesis and properties,
PublikacjaNew azocrown ethers comprising imidazoles in the macrocycle have been synthesized. Imidazole, 2-methyl-, 4-methyl-, and 4-phenylimidazole were incorporated to form macrocyclic units by coupling with the appropriate bis-diazonium salts. The syntheseswere performed under high dilution conditions. The X-ray structure of a water adduct of the 21-membered crown ether derivative of 4-methylimidazole 8 has been solved. Metal...
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Chromogenic Macrocyclic Derivatives of Azoles - Synthesis and Properties
PublikacjaOpisano syntezę makrocyklicznych azokoron zawierających resztę pirolu i imi-dazolu w makropierścieniu. Zbadano zdolność kompleksowania kationów metaliprzez otrzymane związki makrocykliczne przy pomocy spektrofotometrii UV-Visw acetonitrylu. Zbadano także właściwości jonoforowe związków w membranowychelektrodach jonoselektywnych. Ustalono strukturę krystalograficzną 18-czło-nowej pochodnej pirolu.
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Photophysics of 7-Hydroxytetrahydroisoquinoline-3-carboxylic Acid and Its Derivatives
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Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
PublikacjaIn this work, we designed, synthesised and biologically investigated a novel series of 14N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoalkylalcohol we obtained diamino and aminoalkylhydroxy tacrine derivatives. Next, the compounds were acid to give final products 6–13 and 16–21 that were characterised by 1H, 13 C, 31P...
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Synthesis of Novel Phosphonic‐Type Activity‐Based Probes for Neutrophil Serine Proteases and Their Application in Spleen Lysates of Different Organisms
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Solid phase synthesis of two muramyl pentapeptide derivatives
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Synthesis of Thermally Stable Energetic 1,2,3-Triazole Derivatives
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Efficient synthesis of orthogonally protected spermidine and norspermidine derivatives
PublikacjaOtrzymano kilka chronionych pochodnych spermidyny i norspermidyny w wyniku reakcji cyjanoetylowania chronionych diamin, ochrony drugorzędowej grupy aminowej oraz redukcji otrzymanego nitrylu za pomocą wodorku litowo-glinowego w temperaturze 0° C.
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Microwave-assisted synthesis of zinc derivatives of potato starch
PublikacjaZincatated potato starch was prepared in a solid-state, microwave-assisted reaction using generated in situ sodium tetrahydroxozincate [Na2Zn(OH)4]. For comparison, zincatation of starch was also carriedout on convectional heating. Depending on the irradiation conditions, the products of either mono- or crosslinking esterification were formed. Higher power applied at shorter exposition offered products ofmonoesterification, and...
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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
PublikacjaIn 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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Dipodal Tetraamide Derivatives of 1,10-Diaza-18-Crown-6 and Alkylmalonic Acids—Synthesis and Use as Ionophores in Ion Selective Membrane Electrodes
PublikacjaNovel dipodal derivatives of an 18-membered diaza-crown ether with two diamide chains featuring methylmalonic or butylmalonic acid residues were obtained and tested as ionophores in ion-selective plasticized membrane electrodes. The objective of the study was to identify measurement conditions which ensure the most favorable performance for magnesium ion-selective electrodes. The relationship between the molar lipophilic anion...
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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.