Discovery of Coronavirus Main Protease Inhibitors with Enhanced Brain Exposure and Potent Oral Efficacy in SARS-CoV-2 and MERS Infection Models.

Lizzadro L, Li J, Taha TY, Degotte G, Detomasi TC, Zapatero-Belinchon FJ, Hantz ER, Huang S, Matsui Y, Henderson WR, McCann JT, Montano M, Rosecrans J, Torres Pomares DF, McGovern BL, Diaz-Tapia R, Benjamin J, Gordon ME, Suazo ID, Settineri NS, Diallo A, Krogan NJ, Shoichet BK, Verba KA, Albrecht R, García-Sastre A, White KM, Ott M, Craik CS, Renslo AR. Discovery of Coronavirus Main Protease Inhibitors with Enhanced Brain Exposure and Potent Oral Efficacy in SARS-CoV-2 and MERS Infection Models. J Med Chem. 2026 Jan 22; 69(2):1530-1551.