A Quick Route to Multiple Highly Potent SARS‐CoV‐2 Main Protease Inhibitors

• Published in: ChemMedChem Vol. 16; no. 6; pp. 942 - 948
• Main Authors: Yang, Kai S., Ma, Xinyu R., Ma, Yuying, Alugubelli, Yugendar R., Scott, Danielle A., Vatansever, Erol C., Drelich, Aleksandra K., Sankaran, Banumathi, Geng, Zhi Z., Blankenship, Lauren R., Ward, Hannah E., Sheng, Yan J., Hsu, Jason C., Kratch, Kaci C., Zhao, Baoyu, Hayatshahi, Hamed S., Liu, Jin, Li, Pingwei, Fierke, Carol A., Tseng, Chien‐Te K., Xu, Shiqing, Liu, Wenshe Ray
• Format: Journal Article
• Language: English
• Published: WEINHEIM Wiley 18.03.2021; Wiley Subscription Services, Inc; ChemPubSoc Europe
• Subjects: 3C-like protease; 60 APPLIED LIFE SCIENCES; A549 Cells; ACE2; Alanine - analogs & derivatives; Alanine - metabolism; Alanine - pharmacology; Angiotensin-converting enzyme 2; Animals; Antiviral Agents - chemical synthesis; Antiviral Agents - metabolism; Antiviral Agents - pharmacology; Antiviral drugs; antivirals; Catalytic Domain; Chemical bonds; Chemistry, Medicinal; Chlorocebus aethiops; Coronavirus 3C Proteases - antagonists & inhibitors; Coronavirus 3C Proteases - chemistry; Coronavirus 3C Proteases - metabolism; Covalent bonds; COVID-19; Crystallography; Cysteine - chemistry; Cysteine Proteinase Inhibitors - chemical synthesis; Cysteine Proteinase Inhibitors - metabolism; Cysteine Proteinase Inhibitors - pharmacology; Humans; Life Sciences & Biomedicine; main protease; Microbial Sensitivity Tests; Pathogenesis; Pharmacology & Pharmacy; Polypeptides; Protease; Protease inhibitors; Protein Binding; Proteinase inhibitors; Proteolysis; Pyrrolidinones - chemical synthesis; Pyrrolidinones - metabolism; Pyrrolidinones - pharmacology; reversible covalent inhibitors; SARS-CoV-2; SARS-CoV-2 - drug effects; SARS-CoV-2 - enzymology; Science & Technology; Severe acute respiratory syndrome; Severe acute respiratory syndrome coronavirus 2; Vero Cells; Viral diseases; Viruses; COVID-19; 3C-like protease; antivirals; reversible covalent inhibitors; SARS-CoV-2; EFFICACY; main protease; IDENTIFICATION; CORONAVIRUS

The COVID‐19 pathogen, SARS‐CoV‐2, requires its main protease (SC2MPro) to digest two of its translated long polypeptides to form a number of mature proteins that are essential for viral replication and pathogenesis. Inhibition of this vital proteolytic process is effective in preventing the virus f...