Modified Chloropyridyl Ester Derivates as Anti-Mpro Inhibitors for Covid-19 Treatment

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2021-GHOS-69204
Researchers at Purdue University have developed a new class of inhibitors for targeting the main protease (Mpro) of SARS-CoV-2.
There is an unmet need to develop a pharmacological treatment for coronavirus infection that leaves the world faced with an ongoing pandemic and urgent medical crisis. The compounds developed by Purdue researchers in this disclosure are newer modified versions of indole-chloropyridyl ester derivatives that have shown effectiveness as anti-Covid-19 protease inhibitor. One of the compounds, GRL-0920 had anti-viral activity (IC50 = 2.8 micromolar in Vero-E6 cells) as potent as Remdesivir and completely blocked the infectivity and cytopathic effect of SARS-CoV-2 without significant toxicity.

Advantages:
-Novel and Potent Inhibition of Against SARS-CoV-2 Infection
-Drug-Like Properties

Potential Applications:
-Treatment of Covid-19
-Treatment of Coronavirus
-Treatment of Severe Acute Respiratory Syndrome (SARS)
-Pharmaceutical Research and Development

Technology Validation:
Technology was validated in Vero E6 cells and TMPRSS2 (type II transmembrane serine proteases) overexpressing Vero cells.

Recent Publication:
"GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-2-Cov Infection"
American Society of Microbiology
Journal of Molecular Biology and Physiology (mBio)
DOI: 10.1128/mBio.01833-20

"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
Dec 1, 2020
Provisional-Gov. Funding
United States
(None)
(None)

(None)
PCT-Gov. Funding
WO
(None)
(None)
Purdue Office of Technology Commercialization
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Email: otcip@prf.org