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- ISSN: 0929-8665
- E-ISSN: 1875-5305
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Design, Synthesis and Docking Studies of Hydroxyethylamine and Hydroxyethylsulfide BACE-1 Inhibitors
- Source: Protein and Peptide Letters, Volume 16, Issue 1, Jan 2009, p. 86 - 90
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- 01 Jan 2009
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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