Please use this identifier to cite or link to this item: https://dspace.ncfu.ru/handle/20.500.12258/26581
Title: Targeted Synthesis of New 5-Phenyl-2-[(E)-Styryl]-1H-Pyrimidin-6-One Derivatives and Their Inhibitory Activity Toward SARS-CoV-2 Major (MPRO) and Papain-Like Proteases (PLPRO)
Authors: Anenko, D. S.
Аненко, Д. С.
Keywords: Cyclocondensation;X-ray diffraction analysis;N-substituted pyrimidin-6(1H)-one;Pharmacokinetic descriptors;Powder x-ray diffraction;SARS-CoV-2 protease inhibitors;Styrylation
Issue Date: 2023
Citation: Rozhkova, A.S., Kodonidi, I.P., Anenko, D.S., Kirik, S.D., Pozdnyakov, D.I., Filippova, V.P., Vdovenko-Martynova, N.N. Targeted Synthesis of New 5-Phenyl-2-[(E)-Styryl]-1H-Pyrimidin-6-One Derivatives and Their Inhibitory Activity Toward SARS-CoV-2 Major (MPRO) and Papain-Like Proteases (PLPRO) // Pharmaceutical Chemistry Journal. - 2023. - 57 (8). - pp. 1189-1196. - DOI: 10.1007/s11094-024-03025-0
Series/Report no.: Pharmaceutical Chemistry Journal
Abstract: The use of the 5-phenyl-1H-pyrimidin-6-one scaffold in the search for biologically active compounds with antiviral activity based on the pyrimidin-4-one core present in endogenous substances and drugs was substantiated. The molecular activity and pharmacokinetic descriptors for styryl derivatives of N-substituted 5-phenyl-1H-pyrimidin-6-one were predicted in silico via the SwissADME web service. The lack of crystallographic data and information about the tautomeric form of 2,4-dimethyl-5-phenyl-1H-pyrimidin-6-one necessitated the measurement and analysis of x-ray diffraction patterns of the starting substance to explain the reactivity in the styrylation reaction. New derivatives of 5-phenyl-2-[(E)-styryl]-1H-pyrimidin-6-one were synthesized. Studies of their inhibitory activity toward SARS-CoV-2 major (Mpro) and papain-like proteases (PLpro) revealed their marked antiviral activity.
URI: http://hdl.handle.net/20.500.12258/26581
Appears in Collections:Статьи, проиндексированные в SCOPUS, WOS

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