Discovery of a Potent Pyrazolopyridine Series of gamma-Secretase Modulators

作者:Qin Jun*; Zhou Wei; Huang Xianhai; Dhondi Pawan; Palani Anandan; Aslanian Robert; Zhu Zhaoning; Greenlee William; Cohen Williams Mary; Jones Nicholas; Hyde Lynn; Zhang Lili
来源:ACS Medicinal Chemistry Letters, 2011, 2(6): 471-476.
DOI:10.1021/ml2000438

摘要

The synthesis and structure activity relationship of a novel series of pyrazolopyridines are reported. These compounds represent a new class of gamma-secretase modulators that demonstrate good in vitro potency in inhibiting A beta(42) production. Examples with statistically significant in vivo efficacy in reducing the production of rat cerebrospinal fluid A beta(42) were also identified.

  • 出版日期2011-6