1. Academic Validation
  2. Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication

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

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.
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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