Nature Communications (Feb 2023)
Identification of SARS-CoV-2 Mpro inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2
- Nobuyo Higashi-Kuwata,
- Kohei Tsuji,
- Hironori Hayashi,
- Haydar Bulut,
- Maki Kiso,
- Masaki Imai,
- Hiromi Ogata-Aoki,
- Takahiro Ishii,
- Takuya Kobayakawa,
- Kenta Nakano,
- Nobutoki Takamune,
- Naoki Kishimoto,
- Shin-ichiro Hattori,
- Debananda Das,
- Yukari Uemura,
- Yosuke Shimizu,
- Manabu Aoki,
- Kazuya Hasegawa,
- Satoshi Suzuki,
- Akie Nishiyama,
- Junji Saruwatari,
- Yukiko Shimizu,
- Yoshikazu Sukenaga,
- Yuki Takamatsu,
- Kiyoto Tsuchiya,
- Kenji Maeda,
- Kazuhisa Yoshimura,
- Shun Iida,
- Seiya Ozono,
- Tadaki Suzuki,
- Tadashi Okamura,
- Shogo Misumi,
- Yoshihiro Kawaoka,
- Hirokazu Tamamura,
- Hiroaki Mitsuya
Affiliations
- Nobuyo Higashi-Kuwata
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- Kohei Tsuji
- Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
- Hironori Hayashi
- Department of Infectious Diseases, International Research Institute of Disaster Science, Tohoku University
- Haydar Bulut
- Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH
- Maki Kiso
- Division of Virology, Institute of Medical Science, University of Tokyo
- Masaki Imai
- Division of Virology, Institute of Medical Science, University of Tokyo
- Hiromi Ogata-Aoki
- Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH
- Takahiro Ishii
- Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
- Takuya Kobayakawa
- Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
- Kenta Nakano
- Department of Laboratory Animal Medicine, Research Institute, National Center for Global Health and Medicine
- Nobutoki Takamune
- Department of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University
- Naoki Kishimoto
- Department of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University
- Shin-ichiro Hattori
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- Debananda Das
- Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH
- Yukari Uemura
- Center for Clinical Sciences, National Center for Global Health and Medicine
- Yosuke Shimizu
- Center for Clinical Sciences, National Center for Global Health and Medicine
- Manabu Aoki
- Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH
- Kazuya Hasegawa
- Structural Biology Division, Japan Synchrotron Radiation Research Institute
- Satoshi Suzuki
- Department of Infectious Diseases, Tohoku University Graduate School of Medicine
- Akie Nishiyama
- Department of Infectious Diseases, Tohoku University Graduate School of Medicine
- Junji Saruwatari
- Division of Pharmacology and Therapeutics, Graduate School of Pharmaceutical Sciences, Kumamoto University
- Yukiko Shimizu
- Department of Laboratory Animal Medicine, Research Institute, National Center for Global Health and Medicine
- Yoshikazu Sukenaga
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- Yuki Takamatsu
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- Kiyoto Tsuchiya
- AIDS Clinical Center, National Center for Global Health and Medicine
- Kenji Maeda
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- Kazuhisa Yoshimura
- Tokyo Metropolitan Institute of Public Health
- Shun Iida
- Department of Pathology, National Institute of Infectious Diseases
- Seiya Ozono
- Department of Pathology, National Institute of Infectious Diseases
- Tadaki Suzuki
- Department of Pathology, National Institute of Infectious Diseases
- Tadashi Okamura
- Department of Laboratory Animal Medicine, Research Institute, National Center for Global Health and Medicine
- Shogo Misumi
- Department of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University
- Yoshihiro Kawaoka
- Division of Virology, Institute of Medical Science, University of Tokyo
- Hirokazu Tamamura
- Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
- Hiroaki Mitsuya
- Department of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute
- DOI
- https://doi.org/10.1038/s41467-023-36729-0
- Journal volume & issue
-
Vol. 14,
no. 1
pp. 1 – 13
Abstract
Effective antivirals are critical for combatting SARS-CoV-2 infections. Here, the authors develop two orally available small molecules, which specifically inhibit the activity of the SARS-CoV-2 main protease and potently block the infectivity and replication of various SARS-CoV-2 strains in cells and mice.
