Title of article
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives
Author/Authors
Heuisul Park، نويسنده , , Kyeongsik Min، نويسنده , , Hyo Shin Kwak، نويسنده , , Ki Dong Koo، نويسنده , , Dongchul Lim، نويسنده , , Sang-Won Seo، نويسنده , , Jae-Ung Choi، نويسنده , , Bettina Platt، نويسنده , , Deog-Young Choi، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
2900
To page
2904
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799469
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