含新型去甲抑肽素衍生物（2R，3R）-3-氨基-2-羟基-4-（苯硫基）丁酸的β-分泌酶1抑制剂的设计与合成
Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid.
作者信息
Ziora Zyta, Kasai Soko, Hidaka Koushi, Nagamine Ayaka, Kimura Tooru, Hayashi Yoshio, Kiso Yoshiaki
机构信息
Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, 21st Century COE Program, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
出版信息
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1629-33. doi: 10.1016/j.bmcl.2006.12.097. Epub 2007 Jan 8.
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 P(1) position. Finally, Ptns was found as a suitable P(1) moiety for potent BACE1 inhibitor design.
设计、合成并通过立体化学方法确定了一种新型的去甲他汀衍生物——苯硫基去甲他汀[（2R，3R）-3-氨基-2-羟基-4-（苯硫基）丁酸；Ptns]，其含有羟甲基羰基（HMC）等排体。然后，将Ptns引入到β-分泌酶1（BACE1）抑制剂结构的P(1)位。最后，发现Ptns是用于高效BACE1抑制剂设计的合适P(1)部分。
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