4.5 Editorial Material

Novel Halomethylketone Azadipeptides for Treating COVID-19

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 13, Issue 6, Pages 875-876

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.2c00136

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Funding

  1. Agency for Science, Technology and Research (ASTAR), Singapore

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COVID-19, caused by the SARS-CoV-2 coronavirus, has rapidly become a global pandemic with millions of fatalities. The development of antiviral drugs targeting the virus is ongoing, including peptide inhibitor nirmatrelvir and azadipeptide peptidomimetic inhibitors.
COVID-19 is a highly infectious disease caused by the SARS-CoV-2 coronavirus. It rapidly escalated into a global pandemic, causing more than 6 million fatalities by March 2022, a little over 2 years since its emergence in December 2019. The first peptidomimetic coronavirus main protease inhibitor, nirmatrelvir, was granted Emergency Use Authorization by the U.S. FDA on Dec 22, 2021. Less than a month after its patent application, Hoffmann La-Roche scientists filed a patent application describing azadipeptide peptidomimetic inhibitors (WO 2022/043374 A1). This patent highlight reveals the structure-activity relationship of key azadipeptide inhibitors described in the patent.

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