| Literature DB >> 14741251 |
Stephen F Brady1, Satendra Singh, Ming Chih Crouthamel, M Katharine Holloway, Craig A Coburn, Victor M Garsky, Michael Bogusky, Michael W Pennington, Joseph P Vacca, Daria Hazuda, Ming-Tain Lai.
Abstract
An effective approach for enhancing the selectivity of beta-site amyloid precursor protein cleaving enzyme (BACE 1) inhibitors is developed based on the unique features of the S1' pocket of the enzyme. A series of low molecular weight (<600) compounds were synthesized with different moieties at the P1' position. The selectivity of BACE 1 inhibitors versus cathepsin D and renin was enhanced 120-fold by replacing the hydrophobic propyl group with a hydrophilic propionic acid group.Entities:
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Year: 2004 PMID： 14741251 DOI： 10.1016/j.bmcl.2003.11.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823