Literature DB >> 19576765

Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.

Fredrik Wångsell1, Francesco Russo, Jonas Sävmarker, Asa Rosenquist, Bertil Samuelsson, Mats Larhed.   

Abstract

Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC(50) value of 0.23 microM.

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Year:  2009        PMID: 19576765     DOI: 10.1016/j.bmcl.2009.06.065

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.  Tethered aminohydroxylation: synthesis of the β-amino acid of microsclerodermins A and B.

Authors:  Robert D C Pullin; Akshat H Rathi; Ekaterina Y Melikhova; Christian Winter; Amber L Thompson; Timothy J Donohoe
Journal:  Org Lett       Date:  2013-10-16       Impact factor: 6.005

  2 in total

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