关键词: Antiviral Cage compounds Camphor derivatives Influenza

Mesh : Antiviral Agents / chemistry metabolism pharmacology Camphor / chemistry metabolism pharmacology Hemagglutinin Glycoproteins, Influenza Virus / chemistry metabolism Hydrophobic and Hydrophilic Interactions Imines / chemistry Influenza A Virus, H1N1 Subtype / drug effects Molecular Docking Simulation Protein Conformation Structure-Activity Relationship

来  源:   DOI:10.1016/j.ejmech.2016.10.035   PDF(Sci-hub)

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.
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