- Fragment-based discovery and optimization of BACE1 inhibitors.
Fragment-based discovery and optimization of BACE1 inhibitors.
Bioorganic & medicinal chemistry letters (2010-07-27)
James Madden, Jenny R Dod, Robert Godemann, Joachim Kraemer, Myron Smith, Marion Biniszkiewicz, David J Hallett, John Barker, Jane D Dyekjaer, Thomas Hesterkamp
PMID20656487
摘要
A novel series of 2-aminobenzimidazole inhibitors of BACE1 has been discovered using fragment-based drug discovery (FBDD) techniques. The rapid optimization of these inhibitors using structure-guided medicinal chemistry is discussed.