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Start Over Author "Stasi, Luigi" Topic benzamide Topic parkinson's disease treatment
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1. Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.

Author

Ding, Xiao, Dai, Xuedong, Long, Kai, Peng, Cheng, Andreotti, Daniele, Bamborough, Paul, Eatherton, Andrew J., Edge, Colin, Jandu, Karamjit S., Nichols, Paula L., Philps, Oliver J., Stasi, Luigi Piero, Wan, Zehong, Xiang, Jia-Ning, Dong, Kelly, Dossang, Pamela, Ho, Ming-Hsun, Li, Yi, Mensah, Lucy, and Guan, Xiaoming

Subjects
*BENZAMIDE, *DARDARIN, *SUBSTITUENTS (Chemistry), *CHEMICAL derivatives, *PARKINSON'S disease treatment
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. [ABSTRACT FROM AUTHOR]

Published
2017
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