Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 14, Pages 3635-3638Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.04.076
Keywords
beta-secretase; reduced amide; isostere
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A series of beta-site amyloid precursor protein cleaving enzyme (BALE-1) inhibitors containing psi (CH2NH) reduced amide bond were synthesized. Incorporation of this reduced amide isostere as a non-cleavable peptide surrogate afforded inhibitors possessing low nanomolar potencies in both an enzymatic and cell-based assay. (c) 2006 Elsevier Ltd. All rights reserved.
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