Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
作者信息
Wu Yong-Jin, Zhang Yunhui, Good Andrew C, Burton Catherine R, Toyn Jeremy H, Albright Charles F, Macor John E, Thompson Lorin A
机构信息
Neuroscience Discovery Chemistry, Bristol-Myers Squibb Research and Development, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2009 May 15;19(10):2654-60. doi: 10.1016/j.bmcl.2009.03.144. Epub 2009 Apr 5.
PMID:19375914
Abstract
A series of N-((2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification of several 1,3,5-trisubstituted phenylcarboxyamides with potent BACE inhibitory activity.
摘要
Zotero 插件