BACE-1 inhibition by a series of [psi][CH sub(2)NH] reduced amide isosteres

BACE-1 inhibition by a series of [psi][CH sub(2)NH] reduced amide isosteres

A series of beta -site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a [psi](CH sub(2)NH) 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 a...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3635-3638
Hauptverfasser: Coburn, Craig A, Stachel, Shawn J, Jones, Kristen G, Steele, Thomas G, Rush, Diane M, DiMuzio, Jillian, Pietrak, Beth L, Lai, Ming-Tain, Huang, Qian, Lineberger, Janet, Jin, Lixia, Munshi, Sanjeev, Holloway, MKatharine, Espeseth, Amy, Simon, Adam, Hazuda, Daria, Graham, Samuel L, Vacca, Joseph P
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Sprache:eng
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Zusammenfassung:A series of beta -site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a [psi](CH sub(2)NH) 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.04.076