Novel analogues of a nonnucleoside SARS-CoV-2 RdRp inhibitor as potential antivirotics

The RNA-dependent RNA polymerase (RdRp) represents a prominent target in the discovery and development of new antivirotics against RNA viruses, inhibiting the replication process. One of the most targeted RNA viruses of the last years is, without doubt, SARS-CoV-2, the cause of the recent COVID-19 p...

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Published inBeilstein journal of organic chemistry Vol. 20; no. 1; pp. 1029 - 1036
Main Authors Tóth, Luca Julianna, Krejčová, Kateřina, Dejmek, Milan, Žilecká, Eva, Klepetářová, Blanka, Poštová Slavětínská, Lenka, Bouřa, Evžen, Nencka, Radim
Format Journal Article
LanguageEnglish
Published Germany Beilstein-Institut 06.05.2024
Subjects
antivirotics
Chemistry
Full Research Paper
nonnucleotide inhibitor
rna-dependent rna polymerase
sars-cov-2
SARS-CoV-2
nonnucleotide inhibitor
RNA-dependent RNA polymerase
antivirotics
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Summary:The RNA-dependent RNA polymerase (RdRp) represents a prominent target in the discovery and development of new antivirotics against RNA viruses, inhibiting the replication process. One of the most targeted RNA viruses of the last years is, without doubt, SARS-CoV-2, the cause of the recent COVID-19 pandemic. HeE1-2Tyr, a known inhibitor of flaviviral RdRp, has been discovered to also have antiviral potency against this coronavirus. In this study, we report three distinct modifications of HeE1-2Tyr: conversion of the core from a benzothiazole to a benzoxazole moiety and two different scaffold simplifications, respectively. We provide a novel synthetic approach and, in addition, evaluate the final molecules in an in vitro polymerase assay for biological activity.
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ISSN:1860-5397
1860-5397
DOI:10.3762/BJOC.20.91