1.
Bioorg Med Chem Lett
; 20(9): 2837-42, 2010 May 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20347593
RESUMO
With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2' sub-pocket of the enzyme culminated in identification of an analog that potently lowers peripheral Abeta(40) in transgenic mice with a single subcutaneous dose.