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Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives |
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| Authors: | Park Heuisul Min Kyeongsik Kwak Hyo-Shin Koo Ki Dong Lim Dongchul Seo Sang-Won Choi Jae-Ung Platt Bettina Choi Deog-Young |
| Institution: | aDrug Discovery, Research & Development, LG Life Sciences, 104-1 Munji-dong, Yuseong-gu, Daejon 305-380, Republic of Korea bSchool of Medical Sciences, College of Life Sciences and Medicine, University of Aberdeen, Institute of Medical Sciences, Foresterhill, Aberdeen AB25 2ZD, Scotland, UK |
| 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. |
| Keywords: | Alzheimer’s disease BACE-1 Cyclic urea |
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