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Synfacts 2010(5): 0512-0512  
DOI: 10.1055/s-0029-1219644
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a BACE-1 Inhibitor

Contributor(s): Philip Kocienski
C. Björklund, S. Oscarson, K. Benkestock, N. Borkakoti, K. Jansson, J. Lindberg, L. Vrang, A. Hallberg, Å. Rosenquist, B. Samuelsson*
University College Dublin, Ireland; Stockholm University, Medivir AB, Huddinge and Uppsala University, Sweden
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Publication History

Publication Date:
22 April 2010 (online)

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Significance

BACE-1 (β-site amyloid precursor protein cleaving enzyme) is a key enzyme target for the treatment of Alzheimer’s disease. Compound I is a potent inhibitor of BACE-1 that displays >1000 fold selectivity over cathepsin D.