98737-30-5Relevant academic research and scientific papers
Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold
Ciana, Claire-Lise,Siegrist, Romain,Aissaoui, Hamed,Marx, Leo,Racine, Sophie,Meyer, Solange,Binkert, Christoph,De Kanter, Ruben,Fischli, Christoph,Wittlin, Sergio,Boss, Christoph
supporting information, p. 658 - 662 (2013/03/14)
A novel series of anti-malarials, based on a hydroxy-ethyl-amine scaffold, initially identified as peptidomimetic protease inhibitors is described. Combination of the hydroxy-ethyl-amine anti-malarial phramacophore with the known Mannich base pharmacophor
Aspartic protease inhibitors via C1-homologation of peptidic aldehydes and studies on reduced amide isosteres
Braun, Hannes A.,Zall, Andrea,Brockhaus, Manfred,Schütz, Marco,Meusinger, Reinhard,Schmidt, Boris
, p. 7990 - 7993 (2008/03/14)
(R)-Configured isophthalic hydroxyethylamines play an important role in the inhibition of β-secretase (BACE1). We present the synthesis of a number of (S)-configured hydroxyethylamine derivatives via 2-iodoethanol intermediates and the comparison with the
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 105, (2010/02/07)
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.
A Stereocontrolled Synthesis of Hydroxyethylene Dipeptide Isosteres Using Novel, Chiral Aminoalkyl Epoxides and γ-(Aminoalkyl) γ-Lactones
Evans, Ben E.,Rittle, Kenneth E.,Homnick, Carl F.,Springer, James P.,Hirshfield, Jordan,Veber, Daniel F.
, p. 4615 - 4625 (2007/10/02)
A stereocontrolled synthesis of the hydroxyethylene dipeptide isosteric unit 1 is described.This synthesis is capable of providing all eight stereoisomers of 1 and is amenable to variation of substituents R1 and R2.Also described are the novel chiral epoxides 2 and substituted γ-lactones 3, key intermediates in this synthesis having potentially broad application.
