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Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. Epub 2006 May 11.

BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. craig_coburn@merck.com

Abstract

A series of beta-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a 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.

PMID:
16690314
DOI:
10.1016/j.bmcl.2006.04.076
[Indexed for MEDLINE]

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