Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1. / Sokolova, Anastasiya S.; Yarovaya, Оlga I.; Baev, Dmitry S. и др.
в: European Journal of Medicinal Chemistry, Том 127, 15.02.2017, стр. 661-670.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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TY - JOUR
T1 - Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1
AU - Sokolova, Anastasiya S.
AU - Yarovaya, Оlga I.
AU - Baev, Dmitry S.
AU - Shernyukov, Аndrey V.
AU - Shtro, Anna A.
AU - Zarubaev, Vladimir V.
AU - Salakhutdinov, Nariman F.
N1 - Copyright © 2016 Elsevier Masson SAS. All rights reserved.
PY - 2017/2/15
Y1 - 2017/2/15
N2 - A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower.
AB - A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower.
KW - Antiviral
KW - Cage compounds
KW - Camphor derivatives
KW - Influenza
KW - Hemagglutinin Glycoproteins, Influenza Virus/chemistry
KW - Antiviral Agents/chemistry
KW - Structure-Activity Relationship
KW - Influenza A Virus, H1N1 Subtype/drug effects
KW - Imines/chemistry
KW - Camphor/chemistry
KW - Hydrophobic and Hydrophilic Interactions
KW - Protein Conformation
KW - Molecular Docking Simulation
KW - ENTRY INHIBITORS
KW - FUSION
KW - HEMAGGLUTININ
KW - DISCOVERY
KW - A VIRUS
KW - IN-VITRO
KW - CONFORMATIONAL-CHANGE
KW - ANTIVIRAL ACTIVITY
KW - AGENTS
KW - DERIVATIVES
UR - http://www.scopus.com/inward/record.url?scp=85006150304&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2016.10.035
DO - 10.1016/j.ejmech.2016.10.035
M3 - Article
C2 - 27823881
AN - SCOPUS:85006150304
VL - 127
SP - 661
EP - 670
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -
ID: 9560962