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Novel cinnoline-based inhibitors of LRRK2 kinase activity.
Albert W Garofalo
1 ,
Marc Adler ,
Danielle L Aubele ,
Simeon Bowers ,
Maurizio Franzini ,
Erich Goldbach ,
Colin Lorentzen ,
R Jeffrey Neitz ,
Gary D Probst ,
Kevin P Quinn ,
Pam Santiago ,
Hing L Sham ,
Danny Tam ,
Anh P Truong ,
Xiaocong M Ye ,
Zhao Ren
Jan 1 2013
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Abstract
Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of cinnoline-3-carboxamides that are potent against both wild-type and mutant LRRK2 kinase activity in biochemical assays. These compounds are also shown to be potent inhibitors in a cellular assay and to have good to excellent CNS penetration.