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  • Title: Design and synthesis of BACE1 inhibitors containing a novel norstatine derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric acid.
    Author: Ziora Z, Kasai S, Hidaka K, Nagamine A, Kimura T, Hayashi Y, Kiso Y.
    Journal: Bioorg Med Chem Lett; 2007 Mar 15; 17(6):1629-33. PubMed ID: 17251016.
    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 P(1) position. Finally, Ptns was found as a suitable P(1) moiety for potent BACE1 inhibitor design.
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