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J Med Chem. 2008 Jun 12;51(11):3313-7. doi: 10.1021/jm800138h. Epub 2008 May 6.

Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.

Author information

1
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Park, Harlow, Essex, UK.

Abstract

BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.

PMID:
18457381
DOI:
10.1021/jm800138h
[Indexed for MEDLINE]

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