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.
Keywords: Alzheimer, hydrolases, BACE-1, inhibitors, hydroxyethylamine, hydroxyethylsulfide
Protein & Peptide Letters
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:
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.
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Cite this article as:
Rizzi Luca, Vaiana Nadia, Sagui Francesca, Genesio Eva, Pilli Elena, Porcari Valentina and Romeo Sergio, Design, Synthesis and Docking Studies of Hydroxyethylamine and Hydroxyethylsulfide BACE-1 Inhibitors, Protein & Peptide Letters 2009; 16 (1) . https://dx.doi.org/10.2174/092986609787049439
DOI https://dx.doi.org/10.2174/092986609787049439 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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