Discovery of Isonicotinamide Derived β-Secretase Inhibitors: In Vivo Reduction of β-Amyloid
- 21 June 2007
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 50 (15) , 3431-3433
- https://doi.org/10.1021/jm070272d
Abstract
β-Secretase inhibition offers an exciting opportunity for therapeutic intervention in the progression of Alzheimer's disease. A series of isonicotinamides derived from traditional aspartyl protease transition state isostere inhibitors has been optimized to yield low nanomolar inhibitors with sufficient penetration across the blood−brain barrier to demonstrate β-amyloid lowering in a murine model.Keywords
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