SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads

• Published in: Bioorganic & Medicinal Chemistry Letters Vol. 96; p. 129489
• Main Authors: Ghosh, Arun K., Shahabi, Dana, Imhoff, Mackenzie E.C., Kovela, Satish, Sharma, Ashish, Hattori, Shin-ichiro, Higashi-Kuwata, Nobuyo, Mitsuya, Hiroaki, Mesecar, Andrew D.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.11.2023; Elsevier BV
• Subjects: Antiviral; Antiviral Agents; Antiviral Agents - chemistry; Antiviral Agents - pharmacology; COVID-19; Humans; Inhibitor; SARS-CoV-2; SARS-CoV-2 protease; Sulfonamides; Sulfonamides - pharmacology; Synthesis; Antiviral; SARS-CoV-2 protease; Inhibitor; Synthesis; Covid-19

We report here the synthesis and biological evaluation of a series of small molecule SARS-CoV-2 PLpro inhibitors. We compared the activity of selected compounds in both SARS-CoV-1 and SARS-CoV-2 PLpro inhibitory and antiviral assays. We have synthesized and evaluated several new structural variants...