Kohei Tsuji, Takuya Kobayakawa, Takahiro Ishii, Nobuyo Higashi-Kuwata, Chika Azuma, Kouki Shinohara, Yutaro Miura, Kenichi Yamamoto, Soshi Nishimura, Shin-Ichiro Hattori, Haydar Bulut, Hiroaki Mitsuya, Hirokazu Tamamura
In the development of anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) drugs, its main protease (Mpro ), which is an essential enzyme for viral replication, is a promising target. To date, the Mpro inhibitors, nirmatrelvir and ensitrelvir, have been clinically developed by Pfizer Inc. and Shionogi & Co., Ltd., respectively, as orally administrable drugs to treat coronavirus disease of 2019 (COVID-19). We have also developed several potent inhibitors of SARS-CoV-2 Mpro that include compounds 4, 5, TKB245 (6), and TKB248 (7), which possesses a 4-fluorobenzothiazole ketone moiety as a reactive warhead...
2023: Chemical & Pharmaceutical Bulletin