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Updated: Dec 28, 2025
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Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents
Jennifer M Sealy1, Anh P Truong, Luke Tso
1Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, USA.
Abstract:
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Abeta cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1' residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.
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