Structure–Activity Relationship Studies of SARS-CoV‑2 Main Protease Inhibitors Containing 4‑Fluorobenzothiazole-2-carbonyl Moieties

• Published in: Journal of medicinal chemistry Vol. 66; no. 19; pp. 13516 - 13529
• Main Authors: Tsuji, Kohei, Ishii, Takahiro, Kobayakawa, Takuya, Higashi-Kuwata, Nobuyo, Shinohara, Kouki, Azuma, Chika, Miura, Yutaro, Nakano, Hiroki, Wada, Naoya, Hattori, Shin-ichiro, Bulut, Haydar, Mitsuya, Hiroaki, Tamamura, Hirokazu
• Format: Journal Article
• Language: English
• Published: American Chemical Society 12.10.2023

The main protease (Mpro) of SARS-CoV-2 is an attractive target for the development of drugs to treat COVID-19. Here, we report the design, synthesis, and structure–activity relationship (SAR) studies of highly potent SARS-CoV-2 Mpro inhibitors including TKB245 (5)/TKB248 (6). Since we have previousl...