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Updated: Dec 27, 2025
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region
Gary D Probst1, Simeon Bowers, Jennifer M Sealy
1Department of Medicinal Chemistry, Elan Pharmaceuticals, South San Francisco, CA 94080, USA.
Abstract:
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.
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