Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication

  • Viruses. 2021 Aug 11;13(8):1585. doi: 10.3390/v13081585.
Milan Dejmek  1 ,  Eva Konkoľová  1 ,  Luděk Eyer  2  3 ,  Petra Straková  2  3 ,  Pavel Svoboda  2  3  4 ,  Michal Šála  1 ,  Kateřina Krejčová  1 ,  Daniel Růžek  2  3 ,  Evzen Boura  1 ,  Radim Nencka  1
Affiliations
  • 1. Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo náměstí 542/2, 160 00 Praha, Czech Republic.
  • 2. Veterinary Research Institute, Emerging Viral Diseases, Hudcova 296/70, 621 00 Brno, Czech Republic.
  • 3. Institute of Parasitology, Biology Centre of the Czech Academy of Sciences, Branišovská 1160/31, 370 05 České Budějovice, Czech Republic.
  • 4. Department of Pharmacology and Pharmacy, Faculty of Veterinary Medicine, University of Veterinary Sciences Brno, Palackého tř. 1946/1, 612 42 Brno, Czech Republic.
PMID: 34452451 DOI: 10.3390/v13081585
Abstract

SARS-CoV-2 has caused an extensive pandemic of COVID-19 all around the world. Key viral Enzymes are suitable molecular targets for the development of new antivirals against SARS-CoV-2 which could represent potential treatments of the corresponding disease. With respect to its essential role in the replication of viral RNA, RNA-dependent RNA polymerase (RdRp) is one of the prime targets. HeE1-2Tyr and related derivatives were originally discovered as inhibitors of the RdRp of flaviviruses. Here, we present that these pyridobenzothiazole derivatives also significantly inhibit SARS-CoV-2 RdRp, as demonstrated using both polymerase- and cell-based Antiviral assays.

Keywords
COVID-19; RNA-dependent RNA polymerase; SAR-CoV-2; antiviral agents; non-nucleotide inhibitor.
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