Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596111 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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.
Related Topics
Physical Sciences and Engineering
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Organic Chemistry
Authors
Albert W. Garofalo, 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,