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

Authors :
Coburn CA
Stachel SJ
Jones KG
Steele TG
Rush DM
DiMuzio J
Pietrak BL
Lai MT
Huang Q
Lineberger J
Jin L
Munshi S
Katharine Holloway M
Espeseth A
Simon A
Hazuda D
Graham SL
Vacca JP
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Jul 15; Vol. 16 (14), pp. 3635-8. Date of Electronic Publication: 2006 May 11.
Publication Year :
2006

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.

Details

Language :
English
ISSN :
0960-894X
Volume :
16
Issue :
14
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
16690314
Full Text :
https://doi.org/10.1016/j.bmcl.2006.04.076