These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
Preprints are manuscripts made publicly available before they have been submitted for formal peer review and publication. They might contain new research findings or data. Preprints can be a draft or final version of an author's research but must not have been accepted for publication at the time of submission.
submitted on 14.10.2020 and posted on 15.10.2020by Julia Stille, Jevgenijs Tjutrins, Guanyu Wang, Felipe A. Venegas, Christopher Hennecker, Andres Mauricio Rueda, Caitlin E. Miron, Sharon Pinus, Anne Labarre, Jessica Plescia, Mihai Burai Patrascu, Danielle Vlaho, Mitchell Huot, Anthony K Mittermaier, Nicolas Moitessier
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS
outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral
drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro
has been identified as a promising target for the development of antiviral drugs. Previously reported
SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent
inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in design and synthesis which led to
submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a