Novel Halomethylketone Azadipeptides for Treating COVID-19

Novel Halomethylketone Azadipeptides for Treating COVID-19

ACS Medicinal Chemistry Letters

10.1021/acsmedchemlett.2c00136

http://dx.doi.org/10.1021/acsmedchemlett.2c00136

C. S. Brian Chia, Yi Yang See

Biochemistry, Organic Chemistry, drug discovery

27 May 2022

Chia, C. S. B., & See, Y. Y. (2022). Novel Halomethylketone Azadipeptides for Treating COVID-19. ACS Medicinal Chemistry Letters, 13(6), 875–876. https://doi.org/10.1021/acsmedchemlett.2c00136

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.

Publisher Copyright

This research is supported by core funding from: Experimental Drug Development Centre
Grant Reference no. : NRF2021-IE-IECF-001

This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Medicinal Chemistry Letters, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see /doi.org/10.1021/acsmedchemlett.2c00136

https://oar.a-star.edu.sg/communities-collections/articles/19033

1948-5875

Experimental Drug Development Centre