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Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core : Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes
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- Sandgren, Veronica (author)
- Linköpings universitet,Organisk Kemi,Tekniska högskolan
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- Agback, Tatiana (author)
- Medivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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- Johansson, Per-Ola (author)
- Medivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden
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- Elsevier, 2012
- 2012
- English.
- In: Bioorganic & Medicinal Chemistry. - : Elsevier. - 0968-0896 .- 1464-3391. ; 29:14, s. 4377-4389
- Journal article (peer-reviewed)
Abstract
Subject headings
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- A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic and cell-based assays, were observed in this series of target compounds, with the best candidates displaying cell-based IC50 values in the low nanomolar range. As an attempt to improve potency, a phenyl substituent aiming at the S3 subpocket was introduced in the macrocyclic ring. X-ray analyses were performed on selected compounds, and enzyme-inhibitor interactions are discussed.
Keyword
- Alzheimer’s disease; BACE-1 inhibition; Macrocycles; Hydroxyethylamine (HEA) isostere
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- ref (subject category)
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