Title of article
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human β-secretase (BACE1) Original Research Article
Author/Authors
Florian Manzenrieder، نويسنده , , Andreas O. Frank، نويسنده , , Timo Huber، نويسنده , , Cornelia Dorner-Ciossek، نويسنده , , Kay-Eberhard Gottschalk and Horst Kessler، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
8
From page
4136
To page
4143
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 ∼ 12 nM).
Keywords
Alzheimer’s disease , ?-Secretase inhibitors , Phosphino dipeptide (PDP) isostere , BACE1
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2007
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305833
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