| Literature DB >> 17149856 |
Hemaka A Rajapakse1, Philippe G Nantermet, Harold G Selnick, Sanjeev Munshi, Georgia B McGaughey, Stacey R Lindsley, Mary Beth Young, Ming-Tain Lai, Amy S Espeseth, Xiao-Ping Shi, Dennis Colussi, Beth Pietrak, Ming-Chih Crouthamel, Katherine Tugusheva, Qian Huang, Min Xu, Adam J Simon, Lawrence Kuo, Daria J Hazuda, Samuel Graham, Joseph P Vacca.
Abstract
We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme beta-secretase (BACE-1). These novel non-transition-state-derived ligands incorporate a single primary amine to interact with the catalytic aspartates of the target enzyme. Optimization of this series provided inhibitors with intrinsic and functional potency comparable to evolved transition state isostere derived inhibitors of BACE-1.Entities:
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Year: 2006 PMID： 17149856 DOI： 10.1021/jm061046r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446