Enhanced Remdesivir Analogues to Target SARS-CoV-2

Molecules. 2023 Mar 13;28(6):2616. doi: 10.3390/molecules28062616.

Abstract

We report the short synthesis of novel C-nucleoside Remdesivir analogues, their cytotoxicity and an in vitro evaluation against SARS-CoV-2 (CoV2). The described compounds are nucleoside analogues bearing a nitrogen heterocycle as purine analogues. The hybrid structures described herein are designed to enhance the anti-CoV2 activity of Remdesivir. The compounds were evaluated for their cytotoxicity and their anti-CoV2 effect. We discuss the impact of combining both sugar and base modifications on the biological activities of these compounds, their lack of cytotoxicity and their antiviral efficacy.

Keywords: C-nucleoside; SARS-CoV-2; antiviral; phosphate prodrug.

MeSH terms

  • Adenosine Monophosphate / analogs & derivatives
  • Alanine / analogs & derivatives
  • Alanine / pharmacology
  • Alanine / therapeutic use
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use
  • COVID-19 Drug Treatment
  • COVID-19*
  • Humans
  • SARS-CoV-2*

Substances

  • Antiviral Agents
  • Alanine
  • remdesivir
  • Adenosine Monophosphate