Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1

Autor: David A, Candito, Vladimir, Simov, Anmol, Gulati, Solomon, Kattar, Ryan W, Chau, Blair T, Lapointe, Joey L, Methot, Duane E, DeMong, Thomas H, Graham, Ravi, Kurukulasuriya, Mitchell H, Keylor, Ling, Tong, Gregori J, Morriello, John J, Acton, Barbara, Pio, Weiguo, Liu, Jack D, Scott, Michael J, Ardolino, Theodore A, Martinot, Matthew L, Maddess, Xin, Yan, Hakan, Gunaydin, Rachel L, Palte, Spencer E, McMinn, Lisa, Nogle, Hongshi, Yu, Ellen C, Minnihan, Charles A, Lesburg, Ping, Liu, Jing, Su, Laxminarayan G, Hegde, Lily Y, Moy, Janice D, Woodhouse, Robert, Faltus, Tina, Xiong, Paul, Ciaccio, Jennifer A, Piesvaux, Karin M, Otte, Matthew E, Kennedy, David Jonathan, Bennett, Erin F, DiMauro, Matthew J, Fell, Santhosh, Neelamkavil, Harold B, Wood, Peter H, Fuller, J Michael, Ellis
Rok vydání: 2022
Předmět:
Zdroj: Journal of medicinal chemistry. 65(24)
ISSN: 1520-4804
Popis: Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically supported, chemically tractable, and potentially disease-modifying mechanism to treat Parkinson's disease. Herein, we describe the optimization of a novel series of potent, selective, central nervous system (CNS)-penetrant 1-heteroaryl-1
Databáze: OpenAIRE