1589474-08-7Relevant academic research and scientific papers
Difluorophenylglycinols as New Modulators of Proteolytic Processing of Amyloid Precursor Proteins
Chen, Chia-Yu,Liao, Yung-Feng,Chang, Ming-Yun,Hu, Ming-Kuan
, p. 161 - 173 (2014/03/21)
Synthesis and evaluation of difluorophenylglycinols as new modulators of proteolytic processing of the amyloid-β precursor proteins for Alzheimer's therapies were described. A range of N-substituted (R)- and (S)- difluorophenylglycinols, structured on the amino alcohol framework, were explored by incorporating the arylsulfonyl moieties and various N-substituents. Evans' chiral auxiliary strategy was employed for the asymmetric synthesis of these enantiomeric difluorophenylglycinols. Compounds with effects on the γ-secretase inhibition and ERK-mediated signaling pathways were evaluated on cell-based assays. Among them, N-cyclopropylmethyl derivatives R-12c and R-13c showed modest γ-secretase inhibition as well as ERK-dependent activation. A range of N-substituted (R)- and (S)-difluorophenylglycinols, structured on the amino alcohol framework, were explored by incorporating the arylsulfonyl moieties and various N-substituents. Compounds with effects on γ-secretase inhibition and ERK-mediated signaling pathways were evaluated on cell-based assays. The N-cyclopropylmethyl derivatives R-12c and R-13c showed modest γ-secretase inhibition and ERK-dependent activation.
