Peer-reviewed veterinary case report
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2008
- Authors:
- Beswick, Paul et al.
- Affiliation:
- Neurology and Gastrointestinal Centre of Excellence for Drug Discovery · United Kingdom
Abstract
This article is focusing on further optimization of previously described hydroxy ethylamine (HEA) BACE-1 inhibitors obtained from a focused library with the support of X-ray crystallography. Optimization of the non-prime side of our inhibitors and introduction of a 6-membered sultam substituent binding to Asn-294 as well as a fluorine in the C-2 position led to derivatives with nanomolar potency in cell-based assays.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/18171615/