Novel diversity-oriented synthesis-derived respiratory syncytial virus inhibitors identified via a high throughput replicon-based screen

Antiviral Res. 2016 Jul:131:19-25. doi: 10.1016/j.antiviral.2016.03.015. Epub 2016 Apr 6.

Abstract

Respiratory syncytial virus (RSV) infections affect millions of children and adults every year. Despite the significant disease burden, there are currently no safe and effective vaccines or therapeutics. We employed a replicon-based high throughput screen combined with live-virus triaging assays to identify three novel diversity-oriented synthesis-derived scaffolds with activity against RSV. One of these small molecules is shown to target the RSV polymerase (L protein) to inhibit viral replication and transcription; the mechanisms of action of the other small molecules are currently unknown. The compounds described herein may provide attractive inhibitors for lead optimization campaigns.

Keywords: Diversity-oriented synthesis; Replicon; Respiratory syncytial virus.

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / isolation & purification
  • Antiviral Agents / pharmacology*
  • Drug Discovery / methods*
  • Hep G2 Cells
  • High-Throughput Screening Assays / methods*
  • Humans
  • Microbial Sensitivity Tests*
  • RNA-Dependent RNA Polymerase / antagonists & inhibitors
  • Replicon / drug effects*
  • Respiratory Syncytial Virus Infections / therapy
  • Respiratory Syncytial Virus Infections / virology
  • Respiratory Syncytial Virus, Human / drug effects*
  • Respiratory Syncytial Virus, Human / enzymology
  • Respiratory Syncytial Virus, Human / physiology
  • Viral Proteins / antagonists & inhibitors
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Viral Proteins
  • RNA-Dependent RNA Polymerase