Article ID Journal Published Year Pages File Type
5222152 Tetrahedron 2009 13 Pages PDF
Abstract

BACE-1 has emerged as one of the best characterized targets for future Alzheimer therapy. In accordance with the successful identification of masked inhibitors of HIV-1 protease, we envisioned that tert-alcohol containing transition-state mimicking structures would also be worthwhile evaluating as BACE-1 inhibitors. Twelve novel inhibitors were prepared via synthetic routes using epoxyalcohol derivates as key intermediates. The best synthesized tert-hydroxy inhibitor exhibited a BACE-1 IC50 value of 0.38 μM.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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