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J Med Chem. 2006 Dec 14;49(25):7270-3.

Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA. hemaka_rajapakse@merck.com

Abstract

We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme beta-secretase (BACE-1). These novel non-transition-state-derived ligands incorporate a single primary amine to interact with the catalytic aspartates of the target enzyme. Optimization of this series provided inhibitors with intrinsic and functional potency comparable to evolved transition state isostere derived inhibitors of BACE-1.

PMID:
17149856
DOI:
10.1021/jm061046r
[Indexed for MEDLINE]
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