Title: Design, Synthesis and Docking Studies of Hydroxyethylamine and Hydroxyethylsulfide BACE-1 Inhibitors
VOLUME: 16 ISSUE: 1
Author(s):Luca Rizzi, Nadia Vaiana, Francesca Sagui, Eva Genesio, Elena Pilli, Valentina Porcari and Sergio Romeo
Affiliation:Institute of Medicinal Chemistry “Pietro Pratesi”, School of Pharmacy, University of Milan, Via Mangiagalli 25, 20133, Milan (Italy).
Keywords:Alzheimer, hydrolases, BACE-1, inhibitors, hydroxyethylamine, hydroxyethylsulfide
Abstract: Both stereoisomer of hydroxyethylamine (HEA) and hydroxyethylsulfide (HES) transition-state isostere inhibitors of BACE-1 were synthesized. The syn-HEA epimer resulted always more active than the anti stereoisomer independently from the P1 and the P1 substituents. On the contrary, the anti epimer of the HES isostere resulted more active than the syn stereoisomer. The change of stereopreference was studied by molecular modelling.
