Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19

Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19

ACS Medicinal Chemistry Letters

10.1021/acsmedchemlett.2c00349

http://dx.doi.org/10.1021/acsmedchemlett.2c00349

C. S. Brian Chia, Masafumi Inoue

Biochemistry, Organic Chemistry, drug discovery

19 August 2022

Chia, C. S. B., & Inoue, M. (2022). Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19. ACS Medicinal Chemistry Letters, 13(9), 1394–1396. https://doi.org/10.1021/acsmedchemlett.2c00349

The current COVID-19 global pandemic caused by SARS-CoV-2 has claimed more than 6 million lives since its emergence in December 2019. The first oral coronavirus main protease inhibitor, nirmatrelvir, was granted Emergency Use Authorization by the U.S. FDA in December 2021, with a twice-daily dosing regimen in combination with ritonavir. In March 2022, Shionogi & Co. announced their single-agent, once-daily oral SARS-CoV-2 main protease inhibitor, ensitrelvir, was granted approval for global phase 3 clinical trials. Unlike nirmatrelvir, ensitrelvir is a nonpeptidic, noncovalent, small molecule. This Patent Highlight describes key structures and their inhibitory activities in Shionogi & Co.’s and Hokkaido University’s patent WO 2022/138987 A1.

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.2c00349

https://oar.a-star.edu.sg/communities-collections/articles/19036

1948-5875

Experimental Drug Development Centre