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
收藏
页码：1629 / 1633
页数：5
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