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

…, K Hidaka, A Nagamine, T Kimura, Y Hayashi…

Index: Ziora, Zyta; Kasai, Soko; Hidaka, Koushi; Nagamine, Ayaka; Kimura, Tooru; Hayashi, Yoshio; Kiso, Yoshiaki Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1629 - 1633

Full Text: HTML

Citation Number: 11

Abstract

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.