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BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres |
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| Authors: | 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 Katharine Holloway M Espeseth Amy Simon Adam Hazuda Daria Graham Samuel L Vacca Joseph P |
| Affiliation: | 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. |
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