1.
Bioorg Med Chem Lett
; 17(1): 57-62, 2007 Jan 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17055268
RESUMEN
A novel piperidine series of gamma-secretase inhibitors, potentially useful for the treatment of Alzheimer's disease, is disclosed. SAR investigation revealed the requirement for cis-stereochemistry of the substituents attached to the core, which resulted in the chair-like diaxial conformation of the piperidine ring. The series was optimized to provide inhibitors with IC(50)'s in the single-digit nanomolar range. Absolute stereochemistry of the active enantiomer was assigned.