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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; COHENWILLIAMS MARY; JONES NICHOLAS; HYDE LYNN; ZHANG LILI  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2011年2-6;  页码  471-476  
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[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.

 
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