Bifunctional thiosialosides inhibit influenza virus

Bioorg Med Chem Lett. 2014 Jan 15;24(2):636-43. doi: 10.1016/j.bmcl.2013.11.077. Epub 2013 Dec 11.

Abstract

We have synthesized a panel of bivalent S-sialoside analogues, with modifications at the 4 position, as inhibitors of influenza virus. These first generation compounds show IC50 values ranging from low micromolar to high nanomolar in enzyme inhibition and plaque reduction assays with two intact viruses, Influenza H1N1 (A/California/07/2009) and H3N2 (A/Hongkong/8/68).

Keywords: Bifunctional; Glycoconjugates; Influenza virus; Inhibitors; Sialic acid.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology*
  • Humans
  • Influenza A Virus, H1N1 Subtype / drug effects*
  • Influenza A Virus, H1N1 Subtype / physiology
  • Influenza A Virus, H3N2 Subtype / drug effects*
  • Influenza A Virus, H3N2 Subtype / physiology
  • N-Acetylneuraminic Acid / chemistry*
  • N-Acetylneuraminic Acid / pharmacology*

Substances

  • Antiviral Agents
  • N-Acetylneuraminic Acid