Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE

…, JH Toyn, CF Albright, JE Macor, LA Thompson

文献索引：Wu, Yong-Jin; Zhang, Yunhui; Good, Andrew C.; Burton, Catherine R.; Toyn, Jeremy H.; Albright, Charles F.; Macor, John E.; Thompson, Lorin A. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2654 - 2660

全文：HTML全文

被引用次数: 11

摘要

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.