Literature DB >> 17251016

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

Zyta Ziora1, Soko Kasai, Koushi Hidaka, Ayaka Nagamine, Tooru Kimura, Yoshio Hayashi, Yoshiaki Kiso.   

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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Year:  2007        PMID: 17251016     DOI: 10.1016/j.bmcl.2006.12.097

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease.

Authors:  Arun K Ghosh; Heather L Osswald
Journal:  Chem Soc Rev       Date:  2014-10-07       Impact factor: 54.564

2.  Novel entry to the synthesis of (S)- and (R)-5-methoxycarbonylhydroxymethyluridines - a diastereomeric pair of wobble tRNA nucleosides.

Authors:  Robert Borowski; Agnieszka Dziergowska; Elzbieta Sochacka; Grazyna Leszczynska
Journal:  RSC Adv       Date:  2019-12-06       Impact factor: 4.036

  2 in total

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