Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.
Bioorg Med Chem Lett
; 26(1): 51-4, 2016 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-26608551
ABSTRACT
Synthesis, SAR study and BACE1 inhibitory activity of (3S,4S)-4-aminopyrrolidine-3-ol derivatives (2) were described. The compound 7c exhibited more inhibition activity than 11a (IC50 0.05µM vs 0.12µM, respectively), but the latter was more effective in cell-based assay (IC50 1.7µM vs 40% inhibition by 7c @ 10µM) due to the relatively higher cell permeability. Most of the compounds showed high selectivity over BACE2 and cathepsin D. This work will provide useful information for further structural modifications to develop potent BACE1 inhibitors in cell.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Pirrolidinas
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Ácido Aspártico Endopeptidases
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Secretases da Proteína Precursora do Amiloide
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2016
Tipo de documento:
Article