Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.
Bioorg Med Chem Lett
; 27(17): 4034-4038, 2017 09 01.
Article
em En
| MEDLINE
| ID: mdl-28774425
ABSTRACT
Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.
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Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Benzamidas
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Inibidores de Proteínas Quinases
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Descoberta de Drogas
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Serina-Treonina Proteína Quinase-2 com Repetições Ricas em Leucina
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article