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Bioorg Med Chem Lett. 2010 Aug 1;20(15):4639-44. doi: 10.1016/j.bmcl.2010.05.111. Epub 2010 Jun 8.

BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.

Author information

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

Abstract

Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transition state mimetic template. These inhibitors interact with the non prime side of the enzyme using a novel edge-to-face interaction with Arg-296.

PMID:
20579874
DOI:
10.1016/j.bmcl.2010.05.111
[Indexed for MEDLINE]

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