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  • Russo, Francesco, et al. (author)
  • Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors
  • 2009
  • In: Tetrahedron. - : Elsevier BV. - 0040-4020 .- 1464-5416. ; 65:48, s. 10047-10059
  • Journal article (peer-reviewed)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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  • Result 1-1 of 1
Type of publication
journal article (1)
Type of content
peer-reviewed (1)
Author/Editor
Larhed, Mats (1)
Sävmarker, Jonas (1)
Wångsell, Fredrik (1)
Russo, Francesco (1)
Jacobsson, Micael (1)
University
Uppsala University (1)
Language
English (1)
Research subject (UKÄ/SCB)
Medical and Health Sciences (1)
Year
2009 (1)

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