295 research outputs found

    Synthesis and characterisation of nanocrystalline ZrN PVD coatings on AISI 430 stainless steel

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    The nanocrystalline films of zirconium nitride have been synthesized using ion-plasma vacuum-arc deposition technique in combination with high-frequency discharge (RF) on AISI 430 stainless steel at 150oC. Structure examinations X-ray fluorescent analysis (XRF), X-ray diffraction analysis (XRD), scanning electron microscopy (SEM) with microanalysis (EDS), and transmission electron microscopy (TEM), nanoidentation method – were performed to study phase and chemical composition, surface morphology, microstructure and nanohardness of coatings. The developed technology provided low-temperature coatings synthesis, minimized discharge breakdown decreasing formation of macroparticles (MPs) and allowed to deposit ZrN coatings with hardness variation 26.6…31.5 GPa. It was revealed that ZrN single-phase coatings of cubic modification with finecrystalline grains of 20 nm in size were formed

    Anti-corrosion ceramic coatings on the surface of Nd-Fe-B repelling magnets

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    The results of vacuum-arc deposition of thin ZrOβ‚‚coatings to protect the surface of Nd-Fe-B permanent magnets used as repelling devices in orthodontics are presented. The structure, phase composition and mechanical properties of zirconium dioxide films have been investigated by means of SEM, XRD, EDX, XRF and nanoindentation method. It was revealed the formation of polycrystalline ZrOβ‚‚ films of monoclinic modification with average grain size 25 nm. The influence of the ZrOβ‚‚ coating in terms of its barrier properties for corrosion in quasi-physiological 0.9 NaCl solution has been studied. Electrochemical measurements indicated good barrier properties of the coating on specimens in the physiological solution environment

    ΠœΠ΅Ρ‚ΠΈΠ»ΡŽΠ²Π°Π½Π½Ρ полоТСння 8 ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΡ— частини ΠΌΠΎΠ»Π΅ΠΊΡƒΠ»ΠΈ N-(Π±Π΅Π½Π·ΠΈΠ»)-2-гідрокси-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксамідів як спроба посилСння Ρ—Ρ… Π°Π½Π°Π»Π³Π΅Ρ‚ΠΈΡ‡Π½ΠΈΡ… властивостСй

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    The chemical modification of the pyridine moiety of the molecule – displacement of the methyl group in position 8 ofΒ pyrido[1,2-a]pyrimidine nucleus has been considered as one of the possible versions to optimize the biological propertiesΒ of N-(benzyl)-2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamides. The synthesis of the research targetsΒ was carried out by the reaction of the corresponding benzylamines and ethyl 2-hydroxy-8-methyl-4-oxo-4H-pyrido[1,2-a]Β pyrimidine-3-carboxylate, in its turn obtained by condensation of 2-amino-4-methylpyridine (i.e. the product with theΒ methyl group in the intentionally required position) and triethyl methanetricarboxylate. The structure of the compoundsΒ obtained has been confirmed by the data of elemental analysis and NMR 1H spectroscopy, and in the case of opticallyΒ active 1-phenylethylamides additionally by polarimetry. The study of the analgesic properties of all N-(benzyl)-2-hydroxy-8-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamides was performed on the standard experimental β€œacetic acidΒ writhing” model. At the same time, it has been found that our modification is accompanied with the increased biologicalΒ activity of exclusively para-substituted derivatives. For profound research 4-fluorobenzylamide exceeding Piroxicam andΒ Nabumetone by the level of the specific effect has been recommended as a potential new analgesic.Π’ качСствС ΠΎΠ΄Π½ΠΎΠ³ΠΎ ΠΈΠ· Π²ΠΎΠ·ΠΌΠΎΠΆΠ½Ρ‹Ρ… Π²Π°Ρ€ΠΈΠ°Π½Ρ‚ΠΎΠ² ΠΎΠΏΡ‚ΠΈΠΌΠΈΠ·Π°Ρ†ΠΈΠΈ биологичСских свойств N-(Π±Π΅Π½Π·ΠΈΠ»)-2-гидрокси-4-оксо-4Н-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-карбоксамидов рассмотрСна химичСская модификация ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΠΉ части ΠΈΡ… ΠΌΠΎΠ»Π΅ΠΊΡƒΠ»Ρ‹ – ΠΏΠ΅Ρ€Π΅ΠΌΠ΅Ρ‰Π΅Π½ΠΈΠ΅ ΠΌΠ΅Ρ‚ΠΈΠ»ΡŒΠ½ΠΎΠΉ Π³Ρ€ΡƒΠΏΠΏΡ‹ Π² ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½ΠΈΠ΅ 8 ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-a]пиримидинового ядра. Π‘ΠΈΠ½Ρ‚Π΅Π· Ρ†Π΅Π»Π΅Π²Ρ‹Ρ… ΠΎΠ±ΡŠΠ΅ΠΊΡ‚ΠΎΠ² исслСдования осущСствлСн Ρ€Π΅Π°ΠΊΡ†ΠΈΠ΅ΠΉ ΡΠΎΠΎΡ‚Π²Π΅Ρ‚ΡΡ‚Π²ΡƒΡŽΡ‰ΠΈΡ… бСнзиламинов с этил-2-гидрокси-8-ΠΌΠ΅Ρ‚ΠΈΠ»-4-оксо-4Н-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-карбоксилатом, Π² свою ΠΎΡ‡Π΅Ρ€Π΅Π΄ΡŒ, ΠΏΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹ΠΌ кондСнсациСй 2-Π°ΠΌΠΈΠ½ΠΎ-4-ΠΌΠ΅Ρ‚ΠΈΠ»ΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½Π° (Ρ‚. Π΅. ΠΏΡ€ΠΎΠ΄ΡƒΠΊΡ‚Π° с ΠΌΠ΅Ρ‚ΠΈΠ»ΡŒΠ½ΠΎΠΉ Π³Ρ€ΡƒΠΏΠΏΠΎΠΉ Π² Π·Π°Π²Π΅Π΄ΠΎΠΌΠΎ Ρ‚Ρ€Π΅Π±ΡƒΠ΅ΠΌΠΎΠΌ ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½ΠΈΠΈ) с триэтилмСтантрикарбоксилатом. Π‘Ρ‚Ρ€ΠΎΠ΅Π½ΠΈΠ΅ синтСзированных вСщСств ΠΏΠΎΠ΄Ρ‚Π²Π΅Ρ€ΠΆΠ΄Π΅Π½ΠΎ Π΄Π°Π½Π½Ρ‹ΠΌΠΈ элСмСнтного Π°Π½Π°Π»ΠΈΠ·Π° ΠΈ спСктроскопии 1Н ЯМР, Π° Π² случаС оптичСски Π°ΠΊΡ‚ΠΈΠ²Π½Ρ‹Ρ… 1-фСнилэтиламидов Π΄ΠΎΠΏΠΎΠ»Π½ΠΈΡ‚Π΅Π»ΡŒΠ½ΠΎ Π΅Ρ‰Π΅ ΠΈ поляримСтричСски. Π˜Π·ΡƒΡ‡Π΅Π½ΠΈΠ΅ Π°Π½Π°Π»ΡŒΠ³Π΅Ρ‚ΠΈΡ‡Π΅ΡΠΊΠΈΡ… свойств всСх N-(Π±Π΅Π½Π·ΠΈΠ»)-2-гидрокси-8-ΠΌΠ΅Ρ‚ΠΈΠ»-4-оксо-4Н-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-карбоксамидов ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΎ Π½Π° ΡΡ‚Π°Π½Π΄Π°Ρ€Ρ‚Π½ΠΎΠΉΒ ΡΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½ΠΎΠΉ ΠΌΠΎΠ΄Π΅Π»ΠΈ уксуснокислых ΠΊΠΎΡ€Ρ‡Π΅ΠΉ. ΠŸΡ€ΠΈ этом Π½Π°ΠΉΠ΄Π΅Π½ΠΎ, Ρ‡Ρ‚ΠΎ прСдпринятая Π½Π°ΠΌΠΈ модификация сопровоТдаСтся усилСниСм биологичСской активности ΠΈΡΠΊΠ»ΡŽΡ‡ΠΈΡ‚Π΅Π»ΡŒΠ½ΠΎ ΠΏΠ°Ρ€Π°Π·Π°ΠΌΠ΅Ρ‰Π΅Π½Π½Ρ‹Ρ… ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ…. Для ΡƒΠ³Π»ΡƒΠ±Π»Π΅Π½Π½Ρ‹Ρ… испытаний Π² качСствС Π½ΠΎΠ²ΠΎΠ³ΠΎ ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½ΠΎΠ³ΠΎ Π°Π½Π°Π»ΡŒΠ³Π΅Ρ‚ΠΈΠΊΠ° Ρ€Π΅ΠΊΠΎΠΌΠ΅Π½Π΄ΠΎΠ²Π°Π½Β 4-Ρ„Ρ‚ΠΎΡ€Π±Π΅Π½Π·ΠΈΠ»Π°ΠΌΠΈΠ΄, прСвосходящий ΠΏΠΎ ΡƒΡ€ΠΎΠ²Π½ΡŽ спСцифичСского эффСкта ΠŸΠΈΡ€ΠΎΠΊΡΠΈΠΊΠ°ΠΌ ΠΈ НабумСтон.Π―ΠΊ ΠΎΠ΄ΠΈΠ½ Π· ΠΌΠΎΠΆΠ»ΠΈΠ²ΠΈΡ… Π²Π°Ρ€Ρ–Π°Π½Ρ‚Ρ–Π² ΠΎΠΏΡ‚ΠΈΠΌΡ–Π·Π°Ρ†Ρ–Ρ— Π±Ρ–ΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½ΠΈΡ… властивостСй N-(Π±Π΅Π½Π·ΠΈΠ»)-2-гідрокси-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксамідів розглянуто Ρ…Ρ–ΠΌΡ–Ρ‡Π½Ρƒ ΠΌΠΎΠ΄ΠΈΡ„Ρ–ΠΊΠ°Ρ†Ρ–ΡŽ ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΠΎΠ²ΠΎΡ— частини Ρ—Ρ… ΠΌΠΎΠ»Π΅ΠΊΡƒΠ»ΠΈ – пСрСміщСння ΠΌΠ΅Ρ‚ΠΈΠ»ΡŒΠ½ΠΎΡ— Π³Ρ€ΡƒΠΏΠΈ Ρƒ полоТСння 8 ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ ядра. Π‘ΠΈΠ½Ρ‚Π΅Π· Ρ†Ρ–Π»ΡŒΠΎΠ²ΠΈΡ…Β ΠΎΠ±β€™Ρ”ΠΊΡ‚Ρ–Π² дослідТСння здійснСно Ρ€Π΅Π°ΠΊΡ†Ρ–Ρ”ΡŽ Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½ΠΈΡ… Π±Π΅Π½Π·ΠΈΠ»Π°ΠΌΡ–Π½Ρ–Π² Π· Π΅Ρ‚ΠΈΠ»-2-гідрокси-8-ΠΌΠ΅Ρ‚ΠΈΠ»-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксилатом, Ρƒ свою Ρ‡Π΅Ρ€Π³Ρƒ, ΠΎΠ΄Π΅Ρ€ΠΆΠ°Π½ΠΈΠΌ ΠΊΠΎΠ½Π΄Π΅Π½ΡΠ°Ρ†Ρ–Ρ”ΡŽ 2-Π°ΠΌΡ–Π½ΠΎ-4-ΠΌΠ΅Ρ‚ΠΈΠ»ΠΏΡ–Ρ€ΠΈΠ΄ΠΈΠ½ΡƒΒ (Ρ‚ΠΎΠ±Ρ‚ΠΎ ΠΏΡ€ΠΎΠ΄ΡƒΠΊΡ‚Ρƒ Π· ΠΌΠ΅Ρ‚ΠΈΠ»ΡŒΠ½ΠΎΡŽ Π³Ρ€ΡƒΠΏΠΎΡŽ Π² Π·Π°Π²Ρ–Π΄ΠΎΠΌΠΎ Π½Π΅ΠΎΠ±Ρ…Ρ–Π΄Π½ΠΎΠΌΡƒ ΠΏΠΎΠ»ΠΎΠΆΠ΅Π½Π½Ρ–) Π· триСтилмСтантрикарбоксилатом. Π‘ΡƒΠ΄ΠΎΠ²Ρƒ синтСзованих Ρ€Π΅Ρ‡ΠΎΠ²ΠΈΠ½ ΠΏΡ–Π΄Ρ‚Π²Π΅Ρ€Π΄ΠΆΠ΅Π½ΠΎ Π΄Π°Π½ΠΈΠΌΠΈ Π΅Π»Π΅ΠΌΠ΅Π½Ρ‚Π½ΠΎΠ³ΠΎ Π°Π½Π°Π»Ρ–Π·Ρƒ Ρ‚Π° спСктроскопії 1Н ЯМР,Β Π° Ρƒ Π²ΠΈΠΏΠ°Π΄ΠΊΡƒ ΠΎΠΏΡ‚ΠΈΡ‡Π½ΠΎ Π°ΠΊΡ‚ΠΈΠ²Π½ΠΈΡ… 1-Ρ„Π΅Π½Ρ–Π»Π΅Ρ‚ΠΈΠ»Π°ΠΌΡ–Π΄Ρ–Π² Π΄ΠΎΠ΄Π°Ρ‚ΠΊΠΎΠ²ΠΎ Ρ‰Π΅ ΠΉ поляримСтрично. ВивчСння Π°Π½Π°Π»Π³Π΅Ρ‚ΠΈΡ‡Π½ΠΈΡ… властивостСй усіх N-(Π±Π΅Π½Π·ΠΈΠ»)-2-гідрокси-8-ΠΌΠ΅Ρ‚ΠΈΠ»-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксамідів ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΎ Π½Π° стандартній Π΅ΠΊΡΠΏΠ΅Ρ€ΠΈΠΌΠ΅Π½Ρ‚Π°Π»ΡŒΠ½Ρ–ΠΉ ΠΌΠΎΠ΄Π΅Π»Ρ– оцтовокислих ΠΊΠΎΡ€Ρ‡Ρ–Π². ΠŸΡ€ΠΈ Ρ†ΡŒΠΎΠΌΡƒ Π·Π½Π°ΠΉΠ΄Π΅Π½ΠΎ,Β Ρ‰ΠΎ здійснСна Π½Π°ΠΌΠΈ модифікація ΡΡƒΠΏΡ€ΠΎΠ²ΠΎΠ΄ΠΆΡƒΡ”Ρ‚ΡŒΡΡ посилСнням Π±Ρ–ΠΎΠ»ΠΎΠ³Ρ–Ρ‡Π½ΠΎΡ— активності Π²ΠΈΠΊΠ»ΡŽΡ‡Π½ΠΎ ΠΏΠ°Ρ€Π°Π·Π°ΠΌΡ–Ρ‰Π΅Π½ΠΈΡ… ΠΏΠΎΡ…Ρ–Π΄Π½ΠΈΡ…. Для ΠΏΠΎΠ³Π»ΠΈΠ±Π»Π΅Π½ΠΈΡ… Π²ΠΈΠΏΡ€ΠΎΠ±ΠΎΠ²ΡƒΠ²Π°Π½ΡŒ як Π½ΠΎΠ²ΠΈΠΉ ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½ΠΈΠΉ Π°Π½Π°Π»Π³Π΅Ρ‚ΠΈΠΊ Ρ€Π΅ΠΊΠΎΠΌΠ΅Π½

    Some aspects of periodontitis pathogenesis in children.

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    Inflammatory processes in the tissues surrounding tooth root are frequent enough and develop as the direct complication of caries. As acute periodontitis is manifested with grinding toothache and violation of phΒ­yΒ­sioΒ­logical act of chewing, symptoms of general intoxication, the continuous sluggish chronic periodontitis is harmful and dangerous to the organism as well. It forms the state of chronic ΠΎdontogenetic intoxication and chroneosepsis with wrong functioning of some internal organs and body systems. The like complications can cause significant disturbance to the function of kidneys, liver, heart, joints and their treatment without ablating focus of inflammation is often in- effective; this must be taken into account by doctors-interns. However, scanning of the oral cavity by conservative means has its difficulties mostly because of ignoring pathogenesis of such inflammation. That is why activity of ferments of blood dehydrogenases from the periapical tissues of the teeth affected with the chronic periodontitis was studied. The level of succinate dehydrogenase and alpha-glycerophosphate degydrogenase of lymphocytes of 110 schoolchildren aged 13-17 years old was studied. The main group of examined individuals included those of infected with tuberΒ­culousis – 50 individuals, and the control group (60 individuals) – clinically healthy ones without tuberculousis desease. All schoolchildren had 1 or 2 teeth affected with chronic periodontitis of the apical localization. The reΒ­searchers found that a significant inhibition of activity of succinate dehydrogenase and alpha-glycerophosphate degydrogenase ferments occurs in the inflammatory periodontal tissues, which indicates to local immunity decline, and as a consequence, pathogenic bacteria activation. In people infected with tuberculousis these violations were Β more developed. Such features of periodontitis pathogenesis must be taken into account when providing a combined treatment

    RF-Magnetron sputtering of silicon carbide and silicon nitride films for solar cells

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    RF-magnetron nonreactive sputtering method from solid-phase target in argon atmosphere was used for obtaining thin silicon carbide and silicon nitride films, that are used for constructing solar cells based on substrates of single crystal silicon of p-typ

    Vascular mechanism in the formation of diclophenac induced gastrotoxicity: the association with the level of hydrogen sulfide

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    Department of Pharmacology, N. I. Pirogov National Medical University of Vinnitsa, UkraineBackground: Non-steroid anti-inflammatory drugs (NSAIDs)-induced gastrotoxicity arises as a result of imbalance between vasodilator and vasoconstrictor bioregulators. The influence of deficiency and excess of hydrogen sulfide on vascular mechanisms in the formation of NSAIDs-induced gastrotoxicity was investigated. Material and methods: Male nonlinear rats underwent preconditioning with donor of H2S (NaHS) and inhibitor of its synthesis (propargilglycine). Diclophenac sodium was introduced orally (8 mg/kg). In homogenates of rats’ gastric mucosa was evaluated the activity of prostaglandin-H-synthase (PgH-synthase), NO-synthase, content of nitrites and nitrates, H2S and the activity of cystathionine-Ξ³-lyase. In vitro H2S-induced relaxation of mesenteric arteries was measured. Results: Diclophenac sodium decreased cystathionine-Ξ³-lyase enzyme activity, NO-synthase and PGH-synthase (by 17-24%), content of their H2S metabolites and nitrites/nitrates (by 20-22%) in gastric mucosa, and accompanied with the decrease of mesenteric artery sensitivity to vasodilatory action of H2S (EC50 increased to 27.5%). H2S deficiency – increases and excess of H2S – inhibits the negative influence of diclophenac on the production of vasoactive molecules and H2S-induced relaxation of mesenteric arteries. Conclusions: Excess of H2S in organism increases the content of vasoligating molecules and thus can prevent vascular disturbances caused by NSAIDs in rat stomach mucosa

    Temperature influence on the properties of thin Si₃Nβ‚„ films

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    Applying Raman spectroscopy, small-angle x-ray scattering, and atomic force microscopy it were studied phase composition and surface morphology of nanoscale films Si₃Nβ‚„ (obtained by RF magnetron sputtering

    N-Ρ„Π΅Π½Π΅Ρ‚ΠΈΠ»-2-гідрокси-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-Π°]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксаміди як ΠΌΠΎΠΆΠ»ΠΈΠ²Ρ– ΠΏΡ€ΠΎ- тивірусні Π°Π³Π΅Π½Ρ‚ΠΈ

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    Based on the preliminary calculated screening performed by the PASS programme the synthesis of the group of the corresponding N-phenethyl-2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamides as potential antiviral agents has been carried out by the interaction of ethyl esters of 2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxylic acids with 2-arylethylamines in boiling ethanol. Their structure has been confirmed by the data of elemental analysis and NMR 1H spectroscopy. Of the Herpesviruses family such viruses as Herpes Simplex Viruses Type 1 and 2, Varicella-Zoster Virus, Epstein-Barr Virus, as well as Cytomegalovirus have been involved in the screening research. Influenza Virus was presented by two types: A (subtypes H1N1, H3N2, H5N1) and B. The group of viruses affecting different sections of the respiratory tract included Parainfluenza Virus, SARS Virus, Rhinovirus, Adenovirus and Respiratory Syncytial Virus. Besides, Measles Virus, Vaccinia Virus and related Cowpox Virus, Hepatitis B and C Viruses, as well as Venezuelan Equine Encephalitis Virus were involved. The group of viruses causing febrile states of varying severity in human was presented by Rift Valley Fever Virus, West Nile Virus, Yellow Fever Virus, Dengue Virus and Tacaribe Virus. According to the results of the tests performed N-(4-chlorophenethyl)- 2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide has been recommended for further research. Having a low cytotoxicity this compound revealed a high antiviral activity in relation to the West Nile fever virus agent.На основании ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½Π½ΠΎΠ³ΠΎ ΠΏΠΎ ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΌΠ΅ PASS ΠΏΡ€Π΅Π΄Π²Π°Ρ€ΠΈΡ‚Π΅Π»ΡŒΠ½ΠΎΠ³ΠΎ расчСтного скрининга Π² качСствС ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹Ρ… противовирусных Π°Π³Π΅Π½Ρ‚ΠΎΠ² взаимодСйствиСм этиловых эфиров 2-гидрокси-4-оксо-4Н-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-Π°] ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²Ρ‹Ρ… кислот с 2-арилэтиламинами Π² кипящСм этиловом спиртС осущСствлСн синтСз Π³Ρ€ΡƒΠΏΠΏΡ‹ ΡΠΎΠΎΡ‚Π²Π΅Ρ‚ΡΡ‚Π²ΡƒΡŽΡ‰ΠΈΡ… N-Ρ„Π΅Π½Π΅Ρ‚ΠΈΠ»-2-гидрокси-4-оксо-4Н-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ[1,2-Π°]ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-карбоксамидов. Π˜Ρ… строСниС ΠΏΠΎΠ΄Ρ‚Π²Π΅Ρ€ΠΆΠ΄Π΅Π½ΠΎ Π΄Π°Π½Π½Ρ‹ΠΌΠΈ элСмСнтного Π°Π½Π°Π»ΠΈΠ·Π° ΠΈ спСктроскопии ЯМР 1Н. Из сСмСйства гСрпСсвирусов Π² скрининговых исслСдованиях Π±Ρ‹Π»ΠΈ задСйствованы вирусы простого гСрпСса 1 ΠΈ 2 Ρ‚ΠΈΠΏΠΎΠ², вирус Π’Π°Ρ€ΠΈΡ†Π΅Π»Π»Π°-ЗостСра, вирус Π­ΠΏΡˆΡ‚Π΅ΠΉΠ½Π°-Π‘Π°Ρ€Ρ€Π°, Π° Ρ‚Π°ΠΊΠΆΠ΅ цитомСгаловирус. Вирус Π³Ρ€ΠΈΠΏΠΏΠ° Π±Ρ‹Π» прСдставлСн двумя Ρ‚ΠΈΠΏΠ°ΠΌΠΈ: А (ΠΏΠΎΠ΄Ρ‚ΠΈΠΏΡ‹ H1N1, H3N2, H5N1) ΠΈ Π’. Π“Ρ€ΡƒΠΏΠΏΠ° вирусов, ΠΏΠΎΡ€Π°ΠΆΠ°ΡŽΡ‰ΠΈΡ… Ρ€Π°Π·Π»ΠΈΡ‡Π½Ρ‹Π΅ ΠΎΡ‚Π΄Π΅Π»Ρ‹ Π΄Ρ‹Ρ…Π°Ρ‚Π΅Π»ΡŒΠ½ΠΎΠΉ систСмы, Π²ΠΊΠ»ΡŽΡ‡Π°Π»Π° вирус ΠΏΠ°Ρ€Π°Π³Ρ€ΠΈΠΏΠΏΠ°, вирус SARS, риновирус, адСновирус ΠΈ рСспираторный ΡΠΈΠ½Ρ†ΠΈΡ‚ΠΈΠ°Π»ΡŒΠ½Ρ‹ΠΉ вирус. ΠšΡ€ΠΎΠΌΠ΅ Ρ‚ΠΎΠ³ΠΎ, Π±Ρ‹Π»ΠΈ задСйствованы вирусы ΠΊΠΎΡ€ΠΈ, ΠΊΠΎΡ€ΠΎΠ²ΡŒΠ΅ΠΉ оспы, родствСнный Π΅ΠΌΡƒ Cowpox вирус, вирусы Π³Π΅ΠΏΠ°Ρ‚ΠΈΡ‚ΠΎΠ² Π’ ΠΈ Π‘, Π° Ρ‚Π°ΠΊΠΆΠ΅ вирус Π’Π΅Π½Π΅ΡΡƒΡΠ»ΡŒΡΠΊΠΎΠ³ΠΎ конского энцСфалита. Π“Ρ€ΡƒΠΏΠΏΠ° вирусов, Π²Ρ‹Π·Ρ‹Π²Π°ΡŽΡ‰ΠΈΡ… Ρƒ Ρ‡Π΅Π»ΠΎΠ²Π΅ΠΊΠ° Π»ΠΈΡ…ΠΎΡ€Π°Π΄ΠΎΡ‡Π½Ρ‹Π΅ состояния Ρ€Π°Π·Π»ΠΈΡ‡Π½ΠΎΠΉ стСпСни тяТСсти, прСдставлСна вирусом Π»ΠΈΡ…ΠΎΡ€Π°Π΄ΠΊΠΈ Π΄ΠΎΠ»ΠΈΠ½Ρ‹ Π ΠΈΡ„Ρ‚, вирусом Π—Π°ΠΏΠ°Π΄Π½ΠΎΠ³ΠΎ Нила, вирусом ΠΆΠ΅Π»Ρ‚ΠΎΠΉ Π»ΠΈΡ…ΠΎΡ€Π°Π΄ΠΊΠΈ, вирусом Π”Π΅Π½Π³Π΅ ΠΈ вирусом Π’Π°ΠΊΠ°Ρ€ΠΈΠ±Π΅. По Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Π°ΠΌ ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½Π½Ρ‹Ρ… испытаний для дальнСйшСго изучСния Ρ€Π΅ΠΊΠΎΠΌΠ΅Π½Π΄ΠΎΠ²Π°Π½ N-(4-Ρ…Π»ΠΎΡ€Ρ„Π΅Π½Π΅Ρ‚ΠΈΠ»)-2-гидрокси-4- оксо-4H-ΠΏΠΈΡ€ΠΈΠ΄ΠΎ-[1,2-a]ΠΏΠΈΡ€ΠΈΠΌΠΈΠ΄ΠΈΠ½-3-карбоксамид. ΠŸΡ€ΠΈ Π½ΠΈΠ·ΠΊΠΎΠΉ цитотоксичности это соСдинСниС проявило Π²Ρ‹ΡΠΎΠΊΡƒΡŽ ΠΏΡ€ΠΎΡ‚ΠΈΠ²ΠΎΠ²ΠΈΡ€ΡƒΡΠ½ΡƒΡŽ Π°ΠΊΡ‚ΠΈΠ²Π½ΠΎΡΡ‚ΡŒ ΠΏΠΎ ΠΎΡ‚Π½ΠΎΡˆΠ΅Π½ΠΈΡŽ ΠΊ Π²ΠΎΠ·Π±ΡƒΠ΄ΠΈΡ‚Π΅Π»ΡŽ Π»ΠΈΡ…ΠΎΡ€Π°Π΄ΠΊΠΈ Π—Π°ΠΏΠ°Π΄Π½ΠΎΠ³ΠΎ Нила.На підставі ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΎΠ³ΠΎ Π·Π° ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΎΡŽ PASS ΠΏΠΎΠΏΠ΅Ρ€Π΅Π΄Π½ΡŒΠΎΠ³ΠΎ Ρ€ΠΎΠ·Ρ€Π°Ρ…ΡƒΠ½ΠΊΠΎΠ²ΠΎΠ³ΠΎ скринінгу як ΠΏΠΎΡ‚Π΅Π½Ρ†Ρ–ΠΉΠ½Ρ– противірусні Π°Π³Π΅Π½Ρ‚ΠΈ Π²Π·Π°Ρ”ΠΌΠΎΠ΄Ρ–Ρ”ΡŽ Π΅Ρ‚ΠΈΠ»ΠΎΠ²ΠΈΡ… СстСрів 2-гідрокси-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-Π°]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-ΠΊΠ°Ρ€Π±ΠΎΠ½ΠΎΠ²ΠΈΡ… кислот Π· 2-Π°Ρ€ΠΈΠ»Π΅Ρ‚ΠΈΠ»Π°ΠΌΡ–Π½Π°ΠΌΠΈ Ρƒ киплячому Π΅Ρ‚ΠΈΠ»ΠΎΠ²ΠΎΠΌΡƒ спирті здійснСно синтСз Π³Ρ€ΡƒΠΏΠΈ Π²Ρ–Π΄ΠΏΠΎΠ²Ρ–Π΄Π½ΠΈΡ… N-Ρ„Π΅Π½Π΅Ρ‚ΠΈΠ»- 2-гідрокси-4-оксо-4Н-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-Π°]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксамідів. Π‡Ρ… Π±ΡƒΠ΄ΠΎΠ²Π° ΠΏΡ–Π΄Ρ‚Π²Π΅Ρ€Π΄ΠΆΠ΅Π½Π° Π΄Π°Π½ΠΈΠΌΠΈ Π΅Π»Π΅ΠΌΠ΅Π½Ρ‚Π½ΠΎΠ³ΠΎ Π°Π½Π°Π»Ρ–Π·Ρƒ Ρ‚Π° спСктроскопії ЯМР 1Н. Π— сімСйства гСрпСсвірусів Ρƒ скринінгових дослідТСннях Π±ΡƒΠ»ΠΈ задіяні віруси простого гСрпСсу 1 Ρ‚Π° 2 Ρ‚ΠΈΠΏΡ–Π², вірус Π’Π°Ρ€Ρ–Ρ†Π΅Π»Π»Π°-ЗостСра, вірус Π•ΠΏΡˆΡ‚Π΅ΠΉΠ½Π°-Π‘Π°Ρ€Ρ€Π°, Π° Ρ‚Π°ΠΊΠΎΠΆ цитомСгаловірус. Вірус Π³Ρ€ΠΈΠΏΡƒ Π±ΡƒΠ»ΠΎ прСдставлСно Π΄Π²ΠΎΠΌΠ° Ρ‚ΠΈΠΏΠ°ΠΌΠΈ: А (ΠΏΡ–Π΄Ρ‚ΠΈΠΏΠΈ H1N1, H3N2, H5N1) Ρ‚Π° Π’. Π“Ρ€ΡƒΠΏΠ° вірусів, Ρ‰ΠΎ Π²ΠΈΠΊΠ»ΠΈΠΊΠ°ΡŽΡ‚ΡŒ ураТСння Ρ€Ρ–Π·Π½ΠΈΡ… Π²Ρ–Π΄Π΄Ρ–Π»Ρ–Π² Π΄ΠΈΡ…Π°Π»ΡŒΠ½ΠΎΡ— систСми, Π²ΠΊΠ»ΡŽΡ‡Π°Π»Π° вірус ΠΏΠ°Ρ€Π°Π³Ρ€ΠΈΠΏΡƒ, вірус SARS, риновірус, адСновірус Ρ‚Π° рСспіраторний ΡΠΈΠ½Ρ†ΠΈΡ‚Ρ–Π°Π»ΡŒΠ½ΠΈΠΉ вірус. ΠšΡ€Ρ–ΠΌ Ρ‚ΠΎΠ³ΠΎ, Π±ΡƒΠ»ΠΈ задіяні віруси ΠΊΠΎΡ€Ρƒ, коров’ячої віспи, споріднСний ΠΉΠΎΠΌΡƒ Cowpox вірус, віруси Π³Π΅ΠΏΠ°Ρ‚ΠΈΡ‚Ρ–Π² Π’ Ρ– Π‘, Π° Ρ‚Π°ΠΊΠΎΠΆ вірус Π’Π΅Π½Π΅ΡΡƒΠ΅Π»ΡŒΡΡŒΠΊΠΎΠ³ΠΎ ΠΊΡ–Π½ΡΡŒΠΊΠΎΠ³ΠΎ Π΅Π½Ρ†Π΅Ρ„Π°Π»Ρ–Ρ‚Ρƒ. Π“Ρ€ΡƒΠΏΠ° вірусів, Ρ‰ΠΎ Π²ΠΈΠΊΠ»ΠΈΠΊΠ°ΡŽΡ‚ΡŒ Ρƒ людини Π»ΠΈΡ…ΠΎΠΌΠ°Π½ΠΊΠΈ Ρ€Ρ–Π·Π½ΠΎΠ³ΠΎ ступСня тяТкості, прСдставлСна вірусом Π»ΠΈΡ…ΠΎΠΌΠ°Π½ΠΊΠΈ Π΄ΠΎΠ»ΠΈΠ½ΠΈ Π ΠΈΡ„Ρ‚, вірусом Π—Π°Ρ…Ρ–Π΄Π½ΠΎΠ³ΠΎ Нілу, вірусом ΠΆΠΎΠ²Ρ‚ΠΎΡ— Π»ΠΈΡ…ΠΎΠΌΠ°Π½ΠΊΠΈ, вірусом Π”Π΅Π½Π³Π΅ Ρ‚Π° вірусом Π’Π°ΠΊΠ°Ρ€Ρ–Π±Π΅. Π—Π° Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Π°ΠΌΠΈ ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½ΠΈΡ… Π²ΠΈΠΏΡ€ΠΎΠ±ΠΎΠ²ΡƒΠ²Π°Π½ΡŒ для подальшого вивчСння Ρ€Π΅ΠΊΠΎΠΌΠ΅Π½Π΄ΠΎΠ²Π°Π½ΠΎ N-(4-Ρ…Π»ΠΎΡ€Ρ„Π΅Π½Π΅Ρ‚ΠΈΠ»)- 2-гідрокси-4-оксо-4H-ΠΏΡ–Ρ€ΠΈΠ΄ΠΎ[1,2-a]ΠΏΡ–Ρ€ΠΈΠΌΡ–Π΄ΠΈΠ½-3-карбоксамід. ΠŸΡ€ΠΈ Π½ΠΈΠ·ΡŒΠΊΡ–ΠΉ цитотоксичності ця сполука виявила високу противірусну Π°ΠΊΡ‚ΠΈΠ²Π½Ρ–ΡΡ‚ΡŒ ΠΏΠΎ Π²Ρ–Π΄Π½ΠΎΡˆΠ΅Π½Π½ΡŽ Π΄ΠΎ Π·Π±ΡƒΠ΄Π½ΠΈΠΊΠ° Π»ΠΈΡ…ΠΎΠΌΠ°Π½ΠΊΠΈ Π—Π°Ρ…Ρ–Π΄Π½ΠΎΠ³ΠΎ Нілу

    Effect of aluminium on redox-homeostasis of common buckwheat (Fagopyrum esculentum)

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    Common buckwheat is a significant culture in Ukraine, whose importance for food security has increased in recent decades. An important biological feature of buckwheat is the ability of the crop to grow on poor and especially acidic soils. Common buckwheat was sown in Ukraine on the area of 125,000 ha in 2020, mainly in the central part of the country and in the soil-climatic zone Polesie in the north of the country. At the same time, the area under buckwheat cultivation has been steadily decreasing in the last decade, which is due to the low profitability of cultivation on mainly acidic soils. The research was conducted in the field conditions during 2012–2018 in Kiev region, as well as in laboratory conditions. ICP analysis and biochemical methods were used. Yield of buckwheat on light soils of low fertility depends largely on the level of acidity of the soil. On acidic sod-podzolic soils with loam substrate, the aluminum content of the layer is 20–40 cm higher, compared to a layer of 0–20 cm. This is probably one of the reasons why, when the concentration of aluminum in the soil profile is increased, the root system is located mainly in the upper layer of soil with a lower content of aluminum. In this case, the study of the mechanisms of resistance to the action of aluminum on acidic soils is an important component of the cost-effectiveness of crop production in the region. In acidic soils with pH < 5.0, phytotoxic aluminum (Al3+) rapidly inhibits root growth and afterwards negatively affects water and nutrient uptake in plants. Acquiring phytotoxic capacities, in this connection Al ions affect a wide range of cellular and molecular processes, with a consequent reduction in plant growth. In most plant species, reactive oxygen species (ROS) production can also be induced by Al toxicity leading to oxidative damage of biomolecules and biological membranes. We have detected an accumulation of Al ions in leaf tissues of treatment plants after 10 days of exposure. Tissues of F. esculentum roots contained 155.4% of control level of Al and tissues of F. esculentum leaves – 186.2% of control level of Al ions. Significant intensification of O2‒– generation in roots and leaf tissues as a reaction to Al addition to nutrient solution was detected. Increase in antioxidant enzymes activities and non fixed products of lipids peroxidation was characterized as a biochemical defense reaction of F. esculentum over the 10 days of exposure to Al (50 ΞΌM). Thus, the results show that the action of 50 ΞΌM of Al ions activated antioxidant enzymes – SOD and CAT and decreased oxidative processes, thus promotes pro/antioxidant balance of common buckwheat. These mechanisms of redox homeostasis can be triggers of morphological changes in buckwheat plants, which lead to increased crop resistance when growing on acidic soils with high aluminum content. Thus, the resistance of culture to acid soils may be associated with the possibility of increased accumulation of aluminum in the plant’s tissues, as well as in changes in redox homeostasis with subsequent morphological changes, and primarily the formation of the root system in the top layer of soil with a reduced content of aluminum
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