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  1. Article ; Online: Synthesis of Norabietyl and Nordehydroabietyl Imidazolidine-2,4,5-Triones and Their Activity against Tyrosyl-DNA Phosphodiesterase 1

    Kseniya S. Kovaleva / Olga I. Yarovaya / Irina A. Chernyshova / Alexandra L. Zakharenko / Sergey V. Cheresiz / Amirhossein Azimirad / Andrey G. Pokrovsky / Olga I. Lavrik / Nariman F. Salakhutdinov

    Molbank, Vol 2023, Iss 4, p M

    2023  Volume 1743

    Abstract: New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic ...

    Abstract New imidazolidine-2,4,5-triones with norabietic, nordehydroabietic, and adamantane substituents were synthesized by reacting oxalyl chloride and the corresponding ureas, providing good yields. Bioisosteric replacement of the ureide group with a parabanic acid fragment made it possible to increase the solubility of compounds and conduct biological studies. The compounds inhibit the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 in submicromolar concentrations. Cytotoxic concentrations were also studied on the glioblastoma cell line SNB19.
    Keywords resin acids ; TDP1 inhibitors ; heterocyclic compounds ; DNA repair ; parabanic acid ; adamantane ; Inorganic chemistry ; QD146-197
    Language English
    Publishing date 2023-11-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Synthesis and Antiviral Properties of Camphor-Derived Iminothiazolidine-4-Ones and 2,3-Dihydrothiazoles

    Vladislav V. Oreshko / Kseniya S. Kovaleva / Ekaterina D. Mordvinova / Olga I. Yarovaya / Yuri V. Gatilov / Dmitry N. Shcherbakov / Nikolai I. Bormotov / Olga A. Serova / Larisa N. Shishkina / Nariman F. Salakhutdinov

    Molecules, Vol 27, Iss 15, p

    2022  Volume 4761

    Abstract: A set of heterocyclic products was synthesized from natural (+)-camphor and semi-synthetic (−)-camphor. Then, 2-Imino-4-thiazolidinones and 2,3-dihydrothiazoles were obtained using a three-step procedure. For the synthesized compounds, their antiviral ... ...

    Abstract A set of heterocyclic products was synthesized from natural (+)-camphor and semi-synthetic (−)-camphor. Then, 2-Imino-4-thiazolidinones and 2,3-dihydrothiazoles were obtained using a three-step procedure. For the synthesized compounds, their antiviral activity against the vaccinia virus and Marburg virus was studied. New promising agents active against both viruses were found among the tested compounds.
    Keywords monoterpenoids ; monoterpenes ; vaccinia virus ; Marburg virus ; heterocyclic compounds ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2022-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Synthesis and In Vitro Study of Antiviral Activity of Glycyrrhizin Nicotinate Derivatives against HIV-1 Pseudoviruses and SARS-CoV-2 Viruses

    Vladislav V. Fomenko / Nadezhda B. Rudometova / Olga I. Yarovaya / Artem D. Rogachev / Anastasia A. Fando / Anna V. Zaykovskaya / Nina I. Komarova / Dmitry N. Shcherbakov / Oleg V. Pyankov / Andrey G. Pokrovsky / Larisa I. Karpenko / Rinat A. Maksyutov / Nariman F. Salakhutdinov

    Molecules, Vol 27, Iss 295, p

    2022  Volume 295

    Abstract: When developing drugs against SARS-CoV-2, it is important to consider the characteristics of patients with different co-morbidities. People infected with HIV-1 are a particularly vulnerable group, as they may be at a higher risk than the general ... ...

    Abstract When developing drugs against SARS-CoV-2, it is important to consider the characteristics of patients with different co-morbidities. People infected with HIV-1 are a particularly vulnerable group, as they may be at a higher risk than the general population of contracting COVID-19 with clinical complications. For such patients, drugs with a broad spectrum of antiviral activity are of paramount importance. Glycyrrhizinic acid (Glyc) and its derivatives are promising biologically active compounds for the development of such broad-spectrum antiviral agents. In this work, derivatives of Glyc obtained by acylation with nicotinic acid were investigated. The resulting preparation, Glycyvir, is a multi-component mixture containing mainly mono-, di-, tri- and tetranicotinates. The composition of Glycyvir was characterized by HPLC-MS/MS and its toxicity assessed in cell culture. Antiviral activity against three strains of SARS-CoV-2 was tested in vitro on Vero E6 cells by MTT assay. Glycyvir was shown to inhibit SARS-CoV-2 replication in vitro (IC 50 2–8 μM) with an antiviral activity comparable to the control drug Remdesivir. In addition, Glycyvir exhibited marked inhibitory activity against HIV pseudoviruses of subtypes B, A6 and the recombinant form CRF63_02A (IC 50 range 3.9–27.5 µM). The time-dependence of Glycyvir inhibitory activity on HIV pseudovirus infection of TZM-bl cells suggested that the compound interfered with virus entry into the target cell. Glycyvir is a promising candidate as an agent with low toxicity and a broad spectrum of antiviral action.
    Keywords human immunodeficiency virus type 1 ; SARS-CoV-2 ; entry inhibitors ; nicotinates of glycyrrhizic acid ; Organic chemistry ; QD241-441
    Subject code 570
    Language English
    Publishing date 2022-01-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article: One-pot synthesis of 1,5,3-oxathiazepanes via the three-component condensation of primary amines, formaldehyde and 2-mercaptoethanol

    Kovaleva, Kseniya S / Olga I. Yarovaya / Dmitriy S. Fadeev / Nariman F. Salakhutdinov

    Tetrahedron letters. 2017,

    2017  

    Abstract: The three-component condensation reaction of primary amines, formaldehyde and 2–mercaptoethanol using salts of transition and rare earth metals as catalysts was developed to obtain a new 7-membered heterocyclic structural building block, 1,5,3- ... ...

    Abstract The three-component condensation reaction of primary amines, formaldehyde and 2–mercaptoethanol using salts of transition and rare earth metals as catalysts was developed to obtain a new 7-membered heterocyclic structural building block, 1,5,3-oxathiazepanes, in good to excellent yields. The structure of the heterocyclic fragment was confirmed by NMR spectroscopy.
    Keywords beta-mercaptoethanol ; catalysts ; chemical structure ; condensation reactions ; formaldehyde ; metals ; nuclear magnetic resonance spectroscopy ; primary amines ; salts ; synthesis
    Language English
    Size p. .
    Publishing place Elsevier Ltd
    Document type Article
    Note Pre-press version
    ZDB-ID 204287-3
    ISSN 1873-3581 ; 0040-4039
    ISSN (online) 1873-3581
    ISSN 0040-4039
    DOI 10.1016/j.tetlet.2017.03.090
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Synthesis and Antiviral Activity of Camphene Derivatives against Different Types of Viruses

    Anastasiya S. Sokolova / Valentina P. Putilova / Olga I. Yarovaya / Anastasiya V. Zybkina / Ekaterina D. Mordvinova / Anna V. Zaykovskaya / Dmitriy N. Shcherbakov / Iana R. Orshanskaya / Ekaterina O. Sinegubova / Iana L. Esaulkova / Sophia S. Borisevich / Nikolay I. Bormotov / Larisa N. Shishkina / Vladimir V. Zarubaev / Oleg V. Pyankov / Rinat A. Maksyutov / Nariman F. Salakhutdinov

    Molecules, Vol 26, Iss 2235, p

    2021  Volume 2235

    Abstract: To date, the ‘one bug-one drug’ approach to antiviral drug development cannot effectively respond to the constant threat posed by an increasing diversity of viruses causing outbreaks of viral infections that turn out to be pathogenic for humans. ... ...

    Abstract To date, the ‘one bug-one drug’ approach to antiviral drug development cannot effectively respond to the constant threat posed by an increasing diversity of viruses causing outbreaks of viral infections that turn out to be pathogenic for humans. Evidently, there is an urgent need for new strategies to develop efficient antiviral agents with broad-spectrum activities. In this paper, we identified camphene derivatives that showed broad antiviral activities in vitro against a panel of enveloped pathogenic viruses, including influenza virus A/PR/8/34 (H1N1), Ebola virus (EBOV), and the Hantaan virus. The lead-compound 2a , with pyrrolidine cycle in its structure, displayed antiviral activity against influenza virus (IC 50 = 45.3 µM), Ebola pseudotype viruses (IC 50 = 0.12 µM), and authentic EBOV (IC 50 = 18.3 µM), as well as against pseudoviruses with Hantaan virus Gn-Gc glycoprotein (IC 50 = 9.1 µM). The results of antiviral activity studies using pseudotype viruses and molecular modeling suggest that surface proteins of the viruses required for the fusion process between viral and cellular membranes are the likely target of compound 2a . The key structural fragments responsible for efficient binding are the bicyclic natural framework and the nitrogen atom. These data encourage us to conduct further investigations using bicyclic monoterpenoids as a scaffold for the rational design of membrane-fusion targeting inhibitors.
    Keywords camphen ; antiviral agent ; surface protein ; pseudotype viruses ; molecular docking ; Organic chemistry ; QD241-441
    Subject code 500
    Language English
    Publishing date 2021-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article: Development and validation of ultrafast LC–MS/MS method for quantification of anti-influenza agent camphecene in whole rat blood using dried blood spots and its application to pharmacokinetic studies

    Rogachev, Artem D / Andrey G. Pokrovsky / Mikhail V. Khvostov / Nariman F. Salakhutdinov / Olga I. Yarovaya / Sergey V. Ankov / Tatyana G. Tolstikova

    Journal of chromatography. 2016 Nov. 15, v. 1036-1037

    2016  

    Abstract: A fast, selective and sensitive procedure for quantitation of the camphor-based anti-influenza agent camphecene in whole rat blood was developed and validated using dried blood spots and LC–MS/MS. The method was validated according to recommendations of ... ...

    Abstract A fast, selective and sensitive procedure for quantitation of the camphor-based anti-influenza agent camphecene in whole rat blood was developed and validated using dried blood spots and LC–MS/MS. The method was validated according to recommendations of the FDA and EMA in terms of selectivity, linearity, accuracy, precision, recovery, matrix factor, stability, and carry-over. Sample preparation included spotting 20μL of whole blood taken from the tail vein onto the paper, drying and extracting the analyte, followed by evaporation of the solvent and analysis of the residue. HPLC separations were run on a reversed-phase microcolumn; the time of analysis was less than 2min. MS/MS detection was performed on a triple quadrupole mass-spectrometer using multiple reaction monitoring (MRM) mode. Transitions 196.4→122.2/153.3 and 152.2→93.1/107.2 were monitored for camphecene and 2-adamantylamine hydrochloride (internal standard), respectively. The intra- and inter-day precisions and accuracies, matrix factor, carry-over and recovery were within acceptable limits. Despite low extraction recovery (less than 2%), the sensitivity of the method was enough to detect the analyte in the concentration range 50–2500ng/mL. The application of the method was shown in pharmacokinetic studies of camphecene in rats at a dose of 10mg/kg.
    Keywords blood ; caudal vein ; drying ; evaporation ; high performance liquid chromatography ; monitoring ; pharmacokinetics ; rats ; solvents
    Language English
    Dates of publication 2016-1115
    Size p. 136-141.
    Publishing place Elsevier B.V.
    Document type Article
    ISSN 1570-0232
    DOI 10.1016/j.jchromb.2016.10.009
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