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  • Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.

Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.

Bioorganic & medicinal chemistry letters (2005-03-23)
Eric Gundersen, Kristi Fan, Kimberly Haas, Donna Huryn, J Steven Jacobsen, Anthony Kreft, Robert Martone, Scott Mayer, June Sonnenberg-Reines, Shaiu-Ching Sun, Hua Zhou
PMID15780628
ABSTRACT

Alzheimer's disease (AD) is a debilitating disease widely thought to be associated with the accumulation of beta amyloid (Abeta) in the brain. Inhibition of gamma-secretase, one of the enzymes responsible for Abeta production, may be a useful strategy for the treatment of AD. Described below is a series of gamma-secretase inhibitors designed from a scaffold identified by a ROCS [J. Comput. Chem.1996, 17, 1653] search of the corporate database.