Dissemin is shutting down on January 1st, 2025

Published in

Beilstein-Institut, Beilstein Journal of Organic Chemistry, (20), p. 1029-1036, 2024

DOI: 10.3762/bjoc.20.91

Links

Tools

Export citation

Search in Google Scholar

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

This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

Full text: Download

Orange circle
Preprint: archiving restricted
Orange circle
Postprint: archiving restricted
Green circle
Published version: archiving allowed
Data provided by SHERPA/RoMEO

Abstract

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.