GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-CoV-2 Infection

• Published in: mBio Vol. 11; no. 4
• Main Authors: Hattori, Shin-ichiro, Higshi-Kuwata, Nobuyo, Raghavaiah, Jakka, Das, Debananda, Bulut, Haydar, Davis, David A., Takamatsu, Yuki, Matsuda, Kouki, Takamune, Nobutoki, Kishimoto, Naoki, Okamura, Tadashi, Misumi, Shogo, Yarchoan, Robert, Maeda, Kenji, Ghosh, Arun K., Mitsuya, Hiroaki
• Format: Journal Article
• Language: English
• Published: United States American Society for Microbiology 20.08.2020
• Subjects: Amino Acid Sequence; Animals; antiviral agents; Antiviral Agents - pharmacology; Betacoronavirus - drug effects; Betacoronavirus - enzymology; Chlorocebus aethiops; Chloroquine - pharmacology; Coronavirus 3C Proteases; Coronavirus Infections - drug therapy; Coronavirus Infections - virology; COVID-19; Cysteine Endopeptidases - chemistry; Cysteine Endopeptidases - genetics; Cysteine Endopeptidases - metabolism; Indoles - chemistry; Indoles - pharmacology; Indoles - therapeutic use; main protease; Models, Molecular; Molecular Biology and Physiology; Pandemics; Pneumonia, Viral - drug therapy; Pneumonia, Viral - virology; SARS-CoV-2; Vero Cells; Viral Nonstructural Proteins - antagonists & inhibitors; Viral Nonstructural Proteins - chemistry; Viral Nonstructural Proteins - genetics; Viral Nonstructural Proteins - metabolism; COVID-19; SARS-CoV-2; antiviral agents; main protease

Targeting the main protease (M pro ) of SARS-CoV-2, we identified two indole-chloropyridinyl-ester derivatives, GRL-0820 and GRL-0920, active against SARS-CoV-2, employing RNA-qPCR and immunocytochemistry and show that the two compounds exerted potent activity against SARS-CoV-2. While GRL-0820 and...