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, 17 (6), 1629-33

Design and Synthesis of BACE1 Inhibitors Containing a Novel Norstatine Derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric Acid

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Design and Synthesis of BACE1 Inhibitors Containing a Novel Norstatine Derivative (2R,3R)-3-amino-2-hydroxy-4-(phenylthio)butyric Acid

Zyta Ziora et al. Bioorg Med Chem Lett.

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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