Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives

Heuisul Park, Kyeongsik Min, Hyo-Shin Kwak, Ki Dong Koo, Dongchul Lim, Sang-Won Seo, Jae-Ung Choi, Bettina Platt, Deog-Young Choi

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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 languageEnglish
Pages (from-to)2900-2904
Number of pages5
JournalBioorganic & Medicinal Chemistry
Issue number9
Early online date8 Apr 2008
Publication statusPublished - 1 May 2008


  • Alzheimer's disease
  • BACE-1
  • cyclic urea
  • beta-secretase
  • Alzheimers-disease
  • design

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