| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376562 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2′ and combination of SAR display a >100-fold increase in potency with good cellular activity (IC50 = 0.15 μM) relative to the previously reported compound 3.
Graphical abstractCompound 26 showed excellent inhibitory activity against BACE-1, good selectivity over Cathepsin D.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Heuisul Park, Kyeongsik Min, Hyo-Shin Kwak, Ki Dong Koo, Dongchul Lim, Sang-Won Seo, Jae-Ung Choi, Bettina Platt, Deog-Young Choi,