期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 1, 页码 71-74出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.021
关键词
LRRK2; Leucine rich repeat kinase 2; Parkinson's disease; Kinase inhibitors
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. (C) 2012 Elsevier Ltd. All rights reserved.
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