Abstract
We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cellular activity (IC50 = 0.15 mu M) relative to the previously reported compound 3. (C) 2008 Elsevier Ltd. All rights reserved.
Original language | English |
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Pages (from-to) | 2900-2904 |
Number of pages | 5 |
Journal | Bioorganic & Medicinal Chemistry |
Volume | 18 |
Issue number | 9 |
Early online date | 8 Apr 2008 |
DOIs | |
Publication status | Published - 1 May 2008 |
Keywords
- Alzheimer's disease
- BACE-1
- cyclic urea
- beta-secretase
- Alzheimers-disease
- design