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- Russo, Francesco, et al.
(författare)
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Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors
- 2009
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Ingår i: Tetrahedron. - : Elsevier BV. - 0040-4020 .- 1464-5416. ; 65:48, s. 10047-10059
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Tidskriftsartikel (refereegranskat)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 mu M.
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