Discovery of Isonicotinamide Derived -Secretase Inhibitors: In Vivo Reduction of 
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- 作者：Matthew G. Stanton ; Shaun R. Stauffer ; Alison R. Gregro ; Melissa Steinbeiser ; Philippe Nantermet ; Sethu Sankaranarayanan ; Eric A. Price ; Guoxin Wu ; Ming-Chih Crouthamel ; Joan Ellis ; Ming-Tain Lai ; Amy
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：July 26, 2007
- 年：2007
- 卷：50
- 期：15
- 页码：3431 - 3433
- 全文大小：58K
- 年卷期：v.50,no.15(July 26, 2007)
- ISSN：1520-4804
文摘
-Secretase inhibition offers an exciting opportunity fortherapeutic intervention in the progression of Alzheimer's disease. Aseries of isonicotinamides derived from traditional aspartyl proteasetransition state isostere inhibitors has been optimized to yield lownanomolar inhibitors with sufficient penetration across the blood-brainbarrier to demonstrate -amyloid lowering in a murine model.