Researchers have published the latest results in the development of new crown drugs in Science
Last Update: 2021-02-23
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Xinhua Chengdu, February 19 (Reporter He Weiqing) reporters learned from Sichuan University on the 19th, Sichuan University Huaxi Hospital Biological Therapy National Key Laboratory jointly
Kunming Animal Research Institute, published online in Science on the same day entitled "SARS-CoV-2 Mpro resentors with antiviral activity in a transgenic mouse model" research paper. Experimental data on the SARS-CoV-2 infected mouse model of the new crown Mpro inhibitor were publicly reported for the first time.
it is understood that SARS-CoV-2 main protease (Mpro) play a key role in the replication of the new coronavirus, and its unique cutting points are different from the human protease, so it is considered an ideal target for the development of anti-neoproviral drugs. The study was first designed with rational drugs and synthesized into 32 new structural small molecule compounds containing fragments of bicyclic proline, which effectively inhibit SARS-CoV-2Mpro activity (IC50:7.6-748.5nM) in-body. The
team selected MI-23, an enzyme-suppressing representative molecule with the highest activity, and by analyzing its crystal structure with the Mpro complex, they clarified the interaction patterns between inhibitors and Mpro, which is a good explanation of the highly active structural basis of these compounds, which is also consistent with the team's original molecular design ideas.
After evaluating the anti-SARS-CoV-2 virus activity, pharmacogenetic properties and safety of rats at the in vitro cell level of this series of compounds, the research team finally selected two small molecular compounds (MI-09, MI-30) with high activity and good pharmacogenetic properties and safety to carry out in vivo antiviral activity testing. In
mouse models infected with SARS-CoV-2, oral or abdominal injections of MI-09 or MI-30 significantly reduced lung viral load and lung pathological damage.
The study reported a series of highly active new structural new coronavirus Mpro small molecule inhibitors, and elaborated the agents and antiviral effects of these inhibitors at the molecular, cell and animal levels, confirming the potential of these compounds to develop anti-SARS-CoV-2 virus drugs in terms of pharmacological properties and safety.
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