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Novel Coronavirus Main Protease Di- and Tripeptide Inhibitors for Treating COVID-19.

ABSTRACT: COVID-19 is a highly infectious disease caused by SARS-CoV-2. First reported in December 2019, it rapidly escalated into a global pandemic, resulting in over 6.3 million fatalities by July 4, 2022. The first oral coronavirus main protease inhibitor, nirmatrelvir, was granted Emergency Use Authorization by the U.S. FDA in December 2021. It is a tripeptide incorporated with a C-terminal nitrile designed to bind and form a covalent attachment to the SARS-CoV-2 main protease. Shortly after nirmatrelvir's approval, Enanta Pharmaceuticals' peptidomimetic SARS-CoV-2 main protease inhibitor entered clinical trials in February 2022. This patent highlight reports key structures of di- and tripeptide inhibitors described in Enanta Pharmaceuticals' patent WO 2022/020242 A1.

SUBMITTER: Chia CSB

PROVIDER: S-EPMC9465979 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature

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Novel Coronavirus Main Protease Di- and Tripeptide Inhibitors for Treating COVID-19.

Chia C S Brian CSB See Yi Yang YY

ACS medicinal chemistry letters 20220808 9

COVID-19 is a highly infectious disease caused by SARS-CoV-2. First reported in December 2019, it rapidly escalated into a global pandemic, resulting in over 6.3 million fatalities by July 4, 2022. The first oral coronavirus main protease inhibitor, nirmatrelvir, was granted Emergency Use Authorization by the U.S. FDA in December 2021. It is a tripeptide incorporated with a C-terminal nitrile designed to bind and form a covalent attachment to the SARS-CoV-2 main protease. Shortly after nirmatrel ...[more]

PMID: 36105347

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