Design and Synthesis of 2,3,5-Substituted Imidazolidin-4-one Inhibitors of BACE-1

Structure‐based drug design was used to incorporate the traditional hydroxyethyl amine aspartyl protease inhibitor motif into 2,3,5‐substituted imidazolidin‐4‐one structures with good BACE‐1 enzyme inhibitory potency. These compounds represent a promising drug target for Alzheimer′s disease‐modifyin...

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Bibliographic Details
Published in:ChemMedChem 2007-07, Vol.2 (7), p.995-999
Main Authors: Barrow, James C., Rittle, Kenneth E., Ngo, Phung L., Selnick, Harold G., Graham, Samuel L., Pitzenberger, Steven M., McGaughey, Georgia B., Colussi, Dennis, Lai, Ming-Tain, Huang, Qian, Tugusheva, Katherine, Espeseth, Amy S., Simon, Adam J., Munshi, Sanjeev K., Vacca, Joseph P.
Format: Article
Language:English
Subjects:
alzheimer′s disease
Amyloid Precursor Protein Secretases - antagonists & inhibitors
Amyloid Precursor Protein Secretases - chemistry
Aspartic Acid Endopeptidases - antagonists & inhibitors
Aspartic Acid Endopeptidases - chemistry
Binding Sites
Crystallography, X-Ray
drug design
Hydrogen Bonding
Imidazolidines - chemical synthesis
Imidazolidines - chemistry
Imidazolidines - pharmacology
Mass Spectrometry
Models, Molecular
nitrogen heterocycles
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
structure-activity relationships
β-secretase
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Summary:Structure‐based drug design was used to incorporate the traditional hydroxyethyl amine aspartyl protease inhibitor motif into 2,3,5‐substituted imidazolidin‐4‐one structures with good BACE‐1 enzyme inhibitory potency. These compounds represent a promising drug target for Alzheimer′s disease‐modifying therapy and are therefore of interest to the medicinal chemistry community.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200700038