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 Найдено в других БД:Публикации Чарушина В.Н. (28)
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1.
Инвентарный номер: нет.
   

   
    Study of different carbonaceous materials as modifiers of screen-printed carbon electrodes for the triazid as potential antiviral drug / A. V. Ivoilova, N. A. Malakhova, P. N. Mozharovskaia [et al.] // Electroanalysis. - 2022. - Vol. 34, № 11. - P1745-1755
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: In this work a comparative study of Screen-Printed Carbon Electrodes (SPCE) – bare and modified by drop casting with carbonaceous nanomaterials (CNMs) as Multi Walled Carbon Nanotubes (MWCNT), Carbon Black and Functionalized Carbon Black for voltammetric determination of 5-methyl-6-nitro-7-oxo-4,7-dihydro-1,2,4-triazolo[1,5-a]pyrimidinide l-arginine monohydrate (Triazid) as a potential drug with a broad spectrum of antiviral activity is reported. Bare SPCE and CNMs modified SPCE (SPCE/CNMs) have been characterized morphologically by SEM and electrochemically by cyclic voltammetry/electrochemical impedance spectroscopy with [Fe(CN)6]4−/3− as redox probe. Significant improvement of electrochemical performances is achieved with SPCE/CNMs compared with the bare SPCE. Among SPCE/CNMs studied SPCE modified with MWCNT (SPCE/CNT) is characterized by the best combination of electrochemical properties and electroanalytical performance towards TD. The linear dynamic range is 25–200 mg L−1 (R2=0.9975) with the limit of detection – 2.8 mg L−1 Triazid using SPCE/CNT and Square-Wave Voltammetry technique. The developed sensor was successfully used for Triazid determination in the Pharmaceutical Substance “TRIAZID”. The results achieved with SPCE/CNMs after chemical binding of dissolved oxygen in 0.04 M Britton-Robinson buffer+0.04 M Na2SO3 (pH 7.2±0.2) are very useful for further development of cost-effective and time-consuming pharmaceutical routine assay.

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2.
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    The electrochemical behavior’s character of a potential antiviral drug 3-nitro-4-hydroxy-7-methylthio-4H-[1,2,4]triazolo[5,1-c][1,2,4]triazinide monohydrate / P. N. Mozharovskaia, A. V. Ivoilova, R. A. Drokin [и др.] // Chimica Techno Acta. - 2022. - Vol. 9, № 4. - Ст. 20229426
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
NITROHETEROCYCLIC COMPOUNDS -- ANTIVIRAL ACTIVITY -- CYCLIC VOLTAMMETRY
Аннотация: The results of this study of the electrochemical transformation of 3-R-4-hydroxy-1,4-dihydro-7-X-1,2,4-triazolo[5,1-c][1,2,4] obtained by voltammetry are presented. It was found that 3-R-4-hydroxy-1,4-dihydro-7-X-1,2,4-triazolo[5,1-c][1,2,4] derivatives are capable of electrochemical reduction in the potential range of -0.28 to -0.33 V (relative to Ag/AgCl) in Britton-Robinson buffer at pH = 2. The electrochemical behavior of the sodium salt of 3-nitro-4-hydroxy-7-methylthio-4H-[1,2,4]triazolo[5,1-c][1,2,4]triazinide monohydrate (compound 1), which in silico modeling predicted possible biological activity against various tick-borne encephalitis and Coxsackie B3 viruses. At the potentials of the first stage of electroreduction at pH = 2, the main transformation process is the three-electron reduction scheme of the nitro group of compound 1. It was established that compound 1 in an aprotic medium is reduced in ionic form, most likely in the form of an ion pair with the Na+ cation, and in an aqueous medium in the form of a protonated particle. Based on this, a scheme was proposed for the probable electrochemical transformation of the studied compound.

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3.
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    4-Hydroxy-3-nitro-1,4-dihydrotriazolo[5,1-c][1,2,4]triazines: synthesis, antiviral activity, and electrochemical characteristics / R. A. Drokin, E. A. Fesenko, P. N. Mozharovskaia [et al.] // Russian chemical bulletin. - 2022. - Vol. 71, № 11. - P2460-2466
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: A new method for preparation of 4-hydroxy-3-nitro-1,4-dihydrotriazolo[5,1-c][1,2,4]-triazines using 1-nitro-2-morpholinoethylene and 3-diazo-1,2,4-triazoles is proposed. Antiviral activity against the Coxsackie B3 virus and electrochemical transformations of the prepared compounds are studied.

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4.
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    Conditions for the Synthesis of 4,5-Diaryl-3-hydroxy-2,2'-bipyridine-6-carbonitriles by the Reaction of 1,2,4-Triazine-5-carbonitriles with 2-Aminooxazoles / A. Rammohan, A. P. Krinochkin, D. S. Kopchuk [et al.] // Russian Journal of Organic Chemistry. - 2022. - Vol. 58, № 2. - P175-179
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: Various conditions for the inverse electron-demand aza-Diels–Alder reaction in the series of 5-aryl-3-(2-pyridyl)-1,2,4-triazine-5-carbonitriles and 2-amino-4-aryloxazoles to obtain 4,5-diaryl-3-hydroxy-2,2'-bipyridine-6-carbonitriles were tested. Heating in 1,2-dichlorobenzene or under solvent-free conditions were found to be the most effective.

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5.
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    Synthesis and Photoluminescent Properties of 4,5-Diaryl-3-hydroxy- and 3-Methoxypyridine-6-carbonitriles / A. Rammohan, A. P. Krinochkin, D. S. Kopchuk [et al.] // Russian Journal of Organic Chemistry. - 2022. - Vol. 58, № 2. - P180-183
Рубрики: ХИМИЧЕСКИЕ НАУКИ

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6.
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    Synthetic approaches to 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-ones as basic heterocyclic structures of the antiviral drug Riamilovir (“Triazavirin®”) active against SARS-CoV-2 (COVID-19) / G. A. Artem'ev, V. L. Rusinov, D. S. Kopchuk [et al.] // Organic & biomolecular chemistry. - 2022. - Vol. 20, № 9. - P1828-1837
Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
Аннотация: Fragments of 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one are found in many compounds with various types of biological activities, including the antiviral drug Riamilovir (Triazavirin®), which shows activity against SARS-CoV-2 (COVID-19). Therefore, the development of convenient methods for the synthesis of new derivatives of 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one is always in demand. This review systematizes the information on the most common synthetic methods for constructing the 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one heterocyclic system.

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7.
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    Development of drugs with direct antiviral action based on azaheterocyclic systems / V. N. Charushin, V. L. Rusinov, M. V. Varaksin [et al.] // Herald of the Russian academy of sciences. - 2022. - Vol. 92, № 4. - P505-510
Рубрики: ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ
   ХИМИЧЕСКИЕ НАУКИ
Аннотация: This article discusses the results of studies carried out in recent years by a team of scientists from the Postovskii Institute of Organic Synthesis, Ural Branch, Russian Academy of Sciences, in cooperation with the First President of Russia Boris Yeltsin Ural Federal University, Ural State Medical University, Volgograd State Medical University, and other scientific and production organizations of the country to create triazavirin (riamilovir) and other direct etiotropic antiviral drugs based on azaheterocyclic derivatives.

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8.
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    Abnormal push-pull benzo[4,5]imidazo[1,2-a][1,2,3]triazolo[4,5-e]pyrimidine fluorophores in planarized intramolecular charge transfer (PLICT) state: Synthesis, photophysical studies and theoretical calculations / O. S. Taniya, V. V. Fedotov, L. K. Sadieva [et al.] // Dyes and Pigments. - 2022. - Vol. 204. - Ст. 110405
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The combination of excellent luminescence with high solvent polarity effect and aggregation induced emission (AIE) is an ideal combination for creating fluorophores/probes with high microenvironmental sensitivity. However, many push-pull chromophores of the D−A type in common intramolecular charge transfer (ICT) state with a significant solvatochromic effect and AIE activity, have poor luminescent properties. Herein, to overcome this problem by using reactions of nucleophilic aromatic hydrogen substitution (SNH), we have designed a series of novel 4-heteroaryl-substituted 2-aryl-2H-benzo[4,5]imidazo[1,2-a][1,2,3]triazolo[4,5-e]pyrimidine fluorophores possessing a planarized intramolecular charge transfer (PLICT) state. All these fluorophores exhibited high luminescence quantum yields (up to 60%) and large Stokes shift values of up to 7459 cm−1. Among them, the fluorophore 4h was found to exhibit the most pronounced positive solvatochromic effect and the probe 4f exhibited the most pronounced aggregation induced emission characteristics. This AIE behavior was further confirmed by means of time-resolved fluorescence lifetime measurements as well as DFT-assisted geometry optimization studies. In the presence of trifluoroacetic acid (TFA) compound 4h exhibited a well-pronounced acidochromism via visible color change from yellow-green to orange which returned to the original yellow-green solution after the addition of triethylamine (TEA). The Stern-Volmer constant for the probe 4h towards TFA was 38 M−1. Finally, for the compounds 4f, g, h theoretical calculations in the ground and excited states in different solvents were carried out to confirm the PLICT process. Based on all above the herein reported PLICT fluorophores 4a-h can be successfully applied as biological probes and optical switches.

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9.
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    Azolo[5,1-c][1,2,4]triazines and azoloazapurines: synthesis, antimicrobial activity and in silico studies / E. K. Voinkov, R. A. Drokin, V. V. Fedotov [et al.] // ChemistrySelect. - 2022. - Vol. 7, № 5. - Pe202104253
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The present work reports on the synthesis of series of azolo[5,1-c][1,2,4]triazines and derivatives of azoloazapurines. The synthesized compounds were tested in vitro for antibacterial activity against N. gonorrhoeae and antimycotic activity against Trichophyton interdigitale, Epidermophyton floccosum, Microsporum canis and Candida albicans. It was found that 10 compounds of the series of 3-nitroazolo[5,1-c][1,2,4]triazine-4-amines 4 exhibit high antibacterial activity (MIC≤15 μg/ml), but do not exhibit antimycotic activity. For compounds active against N. gonorrhoeae, a biological target was predicted from the pharmacophore search method and homologous modeling was carried out for it. The results of molecular docking using the constructed model of dihydrofolate reductase have a good correlation with in vitro tests. Refined docking showed the similarity of the leading compounds positions in the protein active site. The formation of stable non-covalent bonds of the nitro group with the amino acid residues Lys34/Lys55 makes a major contribution to the orienting effect of ligands.

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10.
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    Direct C–H thiolation of azolopyrimidines in the synthesis of triazavirin® structural analogues / А. A. Akulov, A. I. Silaeva, M. V. Varaksin [et al.] // Современные синтетические методологии для создания лекарственных препаратов и функциональных материалов : сборник тезисов VI Международной конференции. - Екатеринбург, 2022. - Ст. I-33. - P84
Рубрики: ХИМИЧЕСКИЕ НАУКИ
   ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ

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