MODIFIED Discovery of Potent anti-Mpro Inhibitors for Covid-19 Treatment using Alpha-ketoamide Derivatives
Novel alpha-ketoamide derivatives show potent antiviral activity against SARS-CoV-2 by targeting the main protease, offering improved drug-like properties for Covid-19 treatment and pharmaceutical R&D.
Researchers at Purdue University have developed a new class of compounds that target the main protease (Mpro) in SARS-COV-2/Covid-19 infection.
With the world facing the coronavirus (Covid-19) pandemic, there is an immediate need for intensive protection from the severe acute respiratory illness associated with the disease. Currently, there is no effective pharmaceutical treatment available for SARS-COV-2 infection. These compounds developed by Purdue University researchers are newer modified versions of previous alpha-ketoamide derivatives that have shown potency as anti-viral agents against Covid-19. One of the compounds identified showed potent activity (IC50= 4.2micromolar) in SARS-COV-2 infected Vero-E6 cells.
Advantages:
-Excellent Antiviral Activity Against SARS-CoV-2 in Mammalian Cells
-Improved Drug-Like Properties
Potential Applications:
-Treatment of Covid-19
-Treatment of Coronavirus
-Pharmaceutical Research & Development
Technology Validation: The compounds have been validated in Vero-E6 cells.
Recent Publication:
"A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication"
Nature Communication
DOI: 10.1038/s41467-021-20900-6
TRL: 3
Intellectual Property:
Provisional-Gov. Funding, 2020-12-01, United States | NATL-Patent, 2021-11-30, Canada | PCT-Gov. Funding, 2021-11-30, WO | NATL-Patent, 2021-11-30, Europe | NATL-Patent, 2023-05-31, United States | NATL-Patent, N/A, Canada
Keywords: SARS-COV-2 main protease inhibitors, Covid-19 antiviral compounds, alpha-ketoamide derivatives, Mpro inhibitor, coronavirus treatment, Vero-E6 cell validation, indole moiety, virus replication blocker, improved drug-like properties, pharmaceutical R&D