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HBsAg levels as a guide for finite treatment duration of chronic hepatitis B
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01.10.2019 |
Abdurakhmanov D.
Ibragimov E.
Rozina T.
Nikulkina E.
Mazurchik N.
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Clinics and Research in Hepatology and Gastroenterology |
10.1016/j.clinre.2018.12.007 |
0 |
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Quantitative Prediction of Yield in Transglycosylation Reaction Catalyzed by Nucleoside Phosphorylases
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17.08.2018 |
Alexeev C.
Kulikova I.
Gavryushov S.
Tararov V.
Mikhailov S.
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Advanced Synthesis and Catalysis |
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2 |
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© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim Phosphorolytic transglycosylation catalyzed by nucleoside phosphorylases is an important biotechnological process. The reaction is reversible, and the yield of the target nucleoside depends on its concentration at the equilibrium state. We have shown that initial concentrations of the starting compounds and the phosphorolysis equilibrium constants of starting and final glycosides determine concentrations of all the components at the equilibrium state. Based on that, we developed a novel quantitative approach for the prediction of yields in transglycosylation reactions. This method simplifies the choice of reagent concentrations and their ratios for the maximization of the target nucleoside yield. It is advantageous over widely applied blind and cumbersome trial-and-error approach and can reduce the required chemical and energy resources. The described algorithm could also be applied for other equilibrium transfer reactions. (Figure presented.).
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3′-O-Substituted 5-(perylen-3-ylethynyl)-2′-deoxyuridines as tick-borne encephalitis virus reproduction inhibitors
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15.07.2018 |
Proskurin G.
Orlov A.
Brylev V.
Kozlovskaya L.
Chistov A.
Karganova G.
Palyulin V.
Osolodkin D.
Korshun V.
Aralov A.
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European Journal of Medicinal Chemistry |
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5 |
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© 2018 Elsevier Masson SAS A series of analogues of potent antiviral perylene nucleoside dUY11 with methylthiomethyl (MTM), azidomethyl (AZM) and HO-C1–4-alkyl-1,2,3-triazol-1,4-diyl groups at 3′-O-position as well as the two products of copper-free alkyne-azide cycloaddition of the AZM derivative were prepared and evaluated against tick-borne encephalitis virus (TBEV). Four compounds (4, 6, 8a, 8b) showed EC50 ≤ 10 nM, thus appearing the most potent TBEV inhibitors to date. Moreover, these nucleosides have higher lipophilicity (clogP) and increased solubility in aq. DMSO vs. parent compound dUY11.
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Selective Inhibition of Enterovirus A Species Members’ Reproduction by Furano[2, 3-d]pyrimidine Nucleosides Revealed by Antiviral Activity Profiling against (+)ssRNA Viruses
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28.02.2018 |
Kozlovskaya L.
Golinets A.
Eletskaya A.
Orlov A.
Palyulin V.
Kochetkov S.
Alexandrova L.
Osolodkin D.
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ChemistrySelect |
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11 |
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© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim The rational design of broad-spectrum antivirals requires data on antiviral activity of compounds against multiple viruses, which are often not available. We have developed a panel of (+)ssRNA viruses composed of Enterovirus and Flavivirus genera members allowing to study these activity spectra. Antiviral activity profiling of a set of nucleoside analogues revealed N4-hydroxycytidine as an efficient inhibitor of replication of coxsackieviruses and other enteroviruses, but ineffective against tick-borne encephalitis virus. Furano[2, 3-d]pyrimidine nucleosides with n-pentyl or n-hexyl tails showed selective inhibition of Enterovirus A representatives. 5-(Tetradec-1-yn-1-yl)-uridine showed selective inhibition of tick-borne encephalitis virus at the micromolar level.
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