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Bioorg Med Chem. 2007 Jun 15;15(12):4136-43. Epub 2007 Mar 30.

Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).

Author information

1
Department Chemie, Lehrstuhl II für Organische Chemie, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.

Abstract

Phosphino dipeptide (PDP) isosteres are known to be useful analogues of the transition state of metalloprotease substrates. Here we describe the use of this unit for the design of aspartic protease inhibitors. A PDP analogue of OM00-3, a potent BACE1 inhibitor, was synthesized and exhibited high biological activity (IC50 approximately 12 nM).

PMID:
17433698
DOI:
10.1016/j.bmc.2007.03.072
[Indexed for MEDLINE]

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