Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid

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• 作者：Zyta Ziora ; Soko Kasai ; Koushi Hidaka ; Ayaka Nagamine ; Tooru Kimura ; Yoshio Hayashi ; Yoshiaki Kiso
• 关键词：Alzheimer’ ; s disease ; BACE1 inhibitor ; Norstatine ; Hydroxymethylcarbonyl isostere
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March 2007
• 卷：17
• 期：6
• 页码：1629-1633
• 文件大小：391 K

摘要

A novel norstatine derivative, phenylthionorstatine [(2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid; Ptns], containing a hydroxymethylcarbonyl (HMC) isostere was designed, synthesized, and stereochemically determined. Then, Ptns was introduced into the structure of BACE1 inhibitors at the P₁ position. Finally, Ptns was found as a suitable P₁ moiety for potent BACE1 inhibitor design.