| Literature DB >> 17482814 |
Stacey R Lindsley1, Keith P Moore, Hemaka A Rajapakse, Harold G Selnick, Mary Beth Young, Hong Zhu, Sanjeev Munshi, Lawrence Kuo, Georgia B McGaughey, Dennis Colussi, Ming-Chih Crouthamel, Ming-Tain Lai, Beth Pietrak, Eric A Price, Sethu Sankaranarayanan, Adam J Simon, Guy R Seabrook, Daria J Hazuda, Nicole T Pudvah, Jerome H Hochman, Samuel L Graham, Joseph P Vacca, Philippe G Nantermet.
Abstract
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.Entities:
Mesh：
Substances：
Year: 2007 PMID： 17482814 DOI： 10.1016/j.bmcl.2007.04.072
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823