Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 15, Pages 3431-3433Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070272d
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beta-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 beta-amyloid lowering in a murine model.
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