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

被引：10

作者：

Ziora, Zyta ^{[1
]}

Kasai, Soko ^{[1
]}

Hidaka, Koushi ^{[1
]}

Nagamine, Ayaka ^{[1
]}

Kimura, Tooru ^{[1
]}

Hayashi, Yoshio ^{[1
]}

Kiso, Yoshiaki ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Century COE Program 21, Ctr Frontier Res Med Sci, Dept Med Chem,Yamashina Ku, Kyoto 6078412, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 06期

关键词：

Alzheimer's disease; BACE1; inhibitor; norstatine; hydroxy-methylcarbonyl isostere;

D O I：

10.1016/j.bmcl.2006.12.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel norstatine derivative, phenylthionorstatine [(2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid; Pins], containing a hydroxymethylcarbonyl (HMC) isostere was designed, synthesized, and stereochemically determined. Then, Pins was introduced into the structure of BACE1 inhibitors at the P-1 position. Finally, Ptns was found as a suitable P-1 moiety for potent BACE1 inhibitor design. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1629 / 1633

页数：5

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