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  • Title: Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies.
    Author: Tamamura H, Kato T, Otaka A, Fujii N.
    Journal: Org Biomol Chem; 2003 Jul 21; 1(14):2468-73. PubMed ID: 12956063.
    Abstract:
    Several beta-secretase inhibitors were designed based on hydroxyethylamine dipeptide isostere (HDI) structures and were synthesized by a methodology using the aza-Payne rearragement and O,N-acyl transfer reactions to study their structure-activity relationships. Among these pseudopeptides, effective compounds were developed as the first beta-secretase inhibitors containing the HDI transition state mimic with potent enzyme inhibitory activity (IC50 < 100 nM).
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