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1.
Инвентарный номер: нет.
   


   
    Antiviral properties of verdazyls and leucoverdazyls and their activity against group b enteroviruses / A. S. Volobueva, V. V. Zarubaev, T. G. Fedorchenko [et al.] // Russian journal of infection and immunity. - 2023. - Vol. 13, № 1. - P107-118
Рубрики: ХИМИЧЕСКИЕ НАУКИ
   ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ

Кл.слова (ненормированные):
ENTEROVIRUSES -- ENTEROVIRAL INFECTION -- COXSACKIEVIRUS
Аннотация: Enteroviruses are non-enveloped viruses of Enterovirus genus, Picornaviridae family, causing a variety of human diseases: from acute respiratory and intestinal infections to more severe pathologies including poliomyelitis, encephalitis, myocarditis, pancreatitis. Currently, no approved direct-acting antiviral drugs for treatment of enterovirus infections exists, whereas vaccination is available only for prevention of poliomyelitis and enterovirus 71 infection. Therefore, it is promising to conduct a search for inhibitors of enteroviruses life cycle in drug development to treat enterovirus infections. Here, antiviral properties of stable free radicals, verdazyls, and their precursors, leucoverdazyls, were investigated. It has been shown that leucoverdazyls vs verdazyls increased the survival of permissive cell culture infected with coxsackievirus. The activity range of the lead leucoverdazyl against RNA-containing and DNA-containing human viruses (in the viral yield reduction assay) and its proposed mechanism of action (time of addition assay) was studied. The lead compound suppressed reproduction of group B enteroviruses in vitro, with modest activity against influenza A virus and no activity against herpes virus type 1 and adenovirus type 5. The maximum decrease in viral titers was observed upon its addition to infected cells during early and middle stages of the virus life cycle. Thus, we concluded that the studied compound has a pronounced inhibitory activity against group B enteroviruses not belonging to the class of capsid binder inhibitors, without virucidal properties. Previously, we described antioxidant properties of leucoverdazyls. It is known that many viral infections are accompanied by production of reactive oxygen species and oxidative stress, and some compounds with antioxidant properties exhibit antiviral potential. Targeted chemical modifications of leucoverdazyls and further studies of leucoverdazyl mechanism of action as well as in vivo animal studies are needed. However, the results obtained may be useful for future development of new antiviral drugs to treat enteroviral infections.

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2.
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    Expedient synthesis of 1,2,4-triazinyl substituted benzo[c]coumarins via double oxidation strategy / R. F. Fatykhov, I. A. Khalymbadzha, A. D. Sharapov [et al.] // Chimica Techno Acta. - 2023. - Vol. 10, № 2. - P202310205
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
COUMARIN -- 1,2,4-TRIAZINE -- NUCLEOPHILIC SUBSTITUTION OF HYDROGEN
Аннотация: Herein, we report a convenient one-pot synthesis of 1,2,4-triazinyl derivatives of benzocoumarins. The proposed approach consists of the nucleophilic addition of tetrahydrobenzo annulated dimethoxycoumarin to 1,2,4-triazines followed by double oxidation of both dihydrotriazine and tetrahydrobenzo groups with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). The nucleophilic addition of the dimethoxycoumarin to 1,2,4-triazines was carried out in the presence of three-fold excess of methanesulfonic acid in DCM at room temperature. It takes place between positions 8 and 5 of coumarin and 1,2,4-triazine, respectively. The double oxidation step was carried out with 3.6 equivalent of DDQ. Selective oxidation of dihydrotriazine moiety, without affecting the tetrahydrobenzo fragment, was achieved using 1.2 equivalent of tetrachlorobenzoquinone (TCQ). The differences in the oxidation with TCQ and DDQ appear to be related to the higher oxidative potential of DDQ in contrast to TCQ. The advantages of the method are the elimination of the use of transition metals, the availability of starting materials, and the simplicity of the procedure. The proposed approach provides a two-step one-pot protocol for the synthesis of triazinyl benzocoumarins, precursors for the preparation of push-pull pyridinyl chromophore.

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3.
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    Conjugates of 8-[2,2’-bipyridinyl]coumarins as potential chemosensors for Al3+, Cu2+, Cd2+, Zn2+ ions: synthesis and photophysical properties / A. D. Sharapov, R. F. Fatykhov, I. A. Khalymbadzha [et al.] // Chimica Techno Acta. - 2023. - Vol. 10, № 4. - P202310417
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
CHEMOSENSORS -- COUMARINS -- 2,2’-BIPYRIDINES
Аннотация: In this work, we report the synthesis of novel coumarin-bipyridine conjugates using a sequence of C-C coupling reaction between 5,7-dimethoxycoumarins and 3-pyridyl-6-aryl-1,2,4-triazines followed by the Boger reaction with norbornandiene to obtain 8-[2,2'-bipyridyl]-5,7-dimethoxycoumarins. Photophysical properties were investigated for the obtained series of 8-[2,2'-bipyridyl]-5,7-dimethoxycoumarins: absorption and emission wavelength maxima are in the region of 212-296 and 401-410 nm, respectively; Stokes shifts are up to 116 nm, and fluorescence quantum yields are up to 15.0%. It was found that titrating the conjugates with Al3+, Zn2+, and Cd2+ ions results in an increase in the intensity of the emission maxima of the complexes, while the opposite effect was observed in the case of titration with Cu2+ ions. These findings suggest that the studied compounds may be considered as promising chemosensing materials. Finally, a positive solvatochromism of 8-[2,2'-bipyridyl]coumarins and their metal complexes was established. The experimental data are supported by mathematical calculations according to the Lippert-Matagaequation and Kosower diagram.

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4.
Инвентарный номер: нет.
   


   
    Nanocomposite hydrogels for wastewater treatment / V. Madhavi, T. Ramesh, N. B. Reddy, G. V. Zyryanov // AIP conference proceedings. - 2022. - Vol. 2390. - Ст. 020043
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
HYDROGELS -- NANOCOMPOSITES -- NANOTECHNOLOGY
Аннотация: The insufficient access to drinking water is one of the most prevailing problems throughout the world. It is highly essential for future demands to bring wastewater to reusable form. Hence, water purification has been the focus and attention of many scientists and governmental agencies. The combination of adsorption and nanotechnology-oriented approach with conventional treatment methods has offered interesting benefits to treat waste water. During the last decade, hydrogels have been used as potential adsorbents for the removal of different types of water pollutants. The combination of hydrogels and nanomaterials with multifunctional framework leads to the development of hybrid hydrogels that gives synergistic effect to the novel materials. Because of their biocompatibility and ability to mix with other materials, hydrogels coupled with versatile chemical groups with well-defined three-dimensional porous structure were potentially used for removal of toxic pollutants in water. This article briefly reviews the recent progress in nanobased hydrogels with particular emphasis on wastewater treatment applications.

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5.
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    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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6.
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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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7.
Инвентарный номер: нет.
   
   B 68


   
    Blue-light-promoted radical c-h azolation of cyclic nitrones enabled by selectfluor® / A. A. Akulov, M. V. Varaksin, A. N. Tsmokalyuk [et al.] // Green Chemistry. - 2021. - Vol. 23, № 5. - P2049-2057
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: An original approach to achieve the C(sp2)–H azolation of cyclic aldonitrones mediated by Selectfluor® has first been employed. By exploiting a metal-free, visible-light-promoted cross-dehydrogenative C–N coupling reaction between model aldonitrones, 2H-imidazole 1-oxides, and NH-containing azoles, a series of novel azaheterocyclic derivatives have been obtained in yields up to 94%. The elaborated protocol has proved to be appropriate for gram-scale processes and displayed potential for utilization in the synthesis of novel structural analogues of lanabecestat. Besides, mechanistic studies have revealed that this coupling reaction is likely to proceed via a nitroxide-involving radical pathway, encompassing a chain of electron transfer events, such as hydrogen atom transfer (HAT) and single electron transfer (SET).

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8.
Инвентарный номер: нет.
   
   L 79


   
    Liposomes loaded with lipophilic derivative of closo-carborane as a potential boron delivery system for boron neutron capture therapy of tumors / A. R. Tsygankova, D. A. Gruzdev, V. V. Kanygin [et al.] // Mendeleev Communications. - 2021. - Vol. 31, № 5. - P659-661
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
AMIDE -- CLOSO-CARBORANES -- LIPOSOMES -- U87 TUMOR MODEL -- TOXICITY -- BIODISTRIBUTION
Аннотация: Liposomes encapsulated with lipophilic derivative of 1,2-dicarba-closo-dodecaborane have been obtained and tested for toxicity to glioblastoma U87 cells and biodistribution on a U87MG xenograft mouse model. The liposomes are able to penetrate the tumor and provide boron concentration up to 1.5 mmmmg g–1 with tumor-to-muscle ratio up to 2.4.

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9.
Инвентарный номер: нет.
   
   E 27


   
    Effect of polarity of solvent on silanization of halloysite nanoclay using (3-glycidyloxy propyl) trimethoxy silane / A. M. Abu el-Soad, A. V. Pestov, N. A. Martemyanov [et al.] // Journal of inorganic and organometallic polymers and materials. - 2021. - № 31. - P2569–2578
ББК Г
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Аннотация: The grafting of silane groups on clay surfaces has been recently investigated in order to fabricate versatile compounds with new potential applications in materials science and ecological engineering. This work explored the influence of variety of solvents with variable polarity on the silanization of halloysite nanoclay (HNT) surface by (3-Glycidyloxy propyl) trimethoxy silane. To this purpose, the functionalization of HNT by 3-Glycidyloxypropyltrimethoxysilane (GOPTMS) has been conducted in Ethanol (polar protic solvent), Tetrahydrofuran (THF) and Acetonitrile (polar aprotic solvents), and Hexane, 1,4-Dioxane and Toluene (non polar solvents). The silane grafted materials were characterized by using several techniques, including Fourier Transform Infrared Spectroscopy (FT-IR), elemental analysis, Scanning Electron Microscopy (SEM), Thermogravimetry (TGA), X-ray Diffraction Analysis (XRD) and Nitrogen adsorption/desorption isotherms. The largest silane loading has been detected for the hybrid nanomaterials prepared in Hexane as a dispersing medium.

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10.
Инвентарный номер: нет.
   


    Mochulskaya, N. N.
    Antiviral agents – benzazine derivatives / N. N. Mochulskaya, E. V. Nosova, V. N. Charushin // Chemistry of heterocyclic compounds. - 2021. - Vol. 57. - P374–382
Рубрики: ХИМИЧЕСКИЕ НАУКИ
Кл.слова (ненормированные):
BENZAZINES -- QUINAZOLINE -- QUINOLINE -- QUINOXALINE
Аннотация: The review outlines the results of studies of the antiviral activity of quinoline, quinoxaline, and quinazoline derivatives published over the past 5 years. The supplied data indicate the enormous potential of benzazines for the design of effective antiviral drugs.

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