Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1

Anastasiya S. Sokolova, Оlga I. Yarovaya, Dmitry S. Baev, Аndrey V. Shernyukov, Anna A. Shtro, Vladimir V. Zarubaev, Nariman F. Salakhutdinov

Research output: Contribution to journalArticlepeer-review

21 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)661-670
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume127
DOIs
Publication statusPublished - 15 Feb 2017

Keywords

  • Antiviral
  • Cage compounds
  • Camphor derivatives
  • Influenza
  • Hemagglutinin Glycoproteins, Influenza Virus/chemistry
  • Antiviral Agents/chemistry
  • Structure-Activity Relationship
  • Influenza A Virus, H1N1 Subtype/drug effects
  • Imines/chemistry
  • Camphor/chemistry
  • Hydrophobic and Hydrophilic Interactions
  • Protein Conformation
  • Molecular Docking Simulation
  • ENTRY INHIBITORS
  • FUSION
  • HEMAGGLUTININ
  • DISCOVERY
  • A VIRUS
  • IN-VITRO
  • CONFORMATIONAL-CHANGE
  • ANTIVIRAL ACTIVITY
  • AGENTS
  • DERIVATIVES

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