Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5222152 | Tetrahedron | 2009 | 13 Pages |
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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Organic Chemistry
Authors
Francesco Russo, Fredrik WÃ¥ngsell, Jonas Sävmarker, Micael Jacobsson, Mats Larhed,