Discovery of 2-Amide-3-methylester Thiophenes that Target SARS-CoV-2 Mac1 and Repress Coronavirus Replication, Validating Mac1 as an Antiviral Target
Sarah Wazir,
Tomi A. O. Parviainen,
Jessica J. Pfannenstiel
et al.
Abstract:The COVID-19 pandemic caused by severe acute respiratory
syndrome
coronavirus 2 (SARS-CoV-2) virus has made it clear that further development
of antiviral therapies will be needed. Here, we describe small-molecule
inhibitors for SARS-CoV-2 Mac1, which counters ADP-ribosylation-mediated
innate immune responses. Three high-throughput screening hits had
the same 2-amide-3-methylester thiophene scaffold. We studied the
compound binding mode using X-ray crystallography, allowing us to
design analogues. Compound 27 … Show more
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