Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1

James C. Barrow; Kenneth E. Rittle; Phung L. Ngo; Harold G. Selnick; Samuel L. Graham; Steven M. Pitzenberger; Georgia B. McGaughey; Dennis Colussi; Ming Tain Lai; Qian Huang; Katherine Tugusheva; Amy S. Espeseth; Adam J. Simon; Sanjeev K. Munshi; Joseph P. Vacca

doi:10.1002/cmdc.200700038

Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1

James C. Barrow, Kenneth E. Rittle, Phung L. Ngo, Harold G. Selnick, Samuel L. Graham, Steven M. Pitzenberger, Georgia B. McGaughey, Dennis Colussi, Ming Tain Lai, Qian Huang, Katherine Tugusheva, Amy S. Espeseth, Adam J. Simon, Sanjeev K. Munshi, Joseph P. Vacca

Research output: Contribution to journal › Article › peer-review

29 Scopus citations

Abstract

(Chemical Equation Presented) 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.

Original language	English (US)
Pages (from-to)	995-999
Number of pages	5
Journal	ChemMedChem
Volume	2
Issue number	7
DOIs	https://doi.org/10.1002/cmdc.200700038
State	Published - Jul 9 2007
Externally published	Yes

Keywords

Alzheimer's disease
Drug design
Nitrogen heterocycles
Structure-activity relationships
β-secretase

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Drug Discovery
Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

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Barrow, J. C., Rittle, K. E., Ngo, P. L., Selnick, H. G., Graham, S. L., Pitzenberger, S. M., McGaughey, G. B., Colussi, D., Lai, M. T., Huang, Q., Tugusheva, K., Espeseth, A. S., Simon, A. J., Munshi, S. K., & Vacca, J. P. (2007). Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1. ChemMedChem, 2(7), 995-999. https://doi.org/10.1002/cmdc.200700038

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abstract = "(Chemical Equation Presented) 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.",

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AU - Barrow, James C.

AU - Rittle, Kenneth E.

AU - Ngo, Phung L.

AU - Selnick, Harold G.

AU - Graham, Samuel L.

AU - Pitzenberger, Steven M.

AU - McGaughey, Georgia B.

AU - Colussi, Dennis

AU - Lai, Ming Tain

AU - Huang, Qian

AU - Tugusheva, Katherine

AU - Espeseth, Amy S.

AU - Simon, Adam J.

AU - Munshi, Sanjeev K.

AU - Vacca, Joseph P.

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AB - (Chemical Equation Presented) 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.

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KW - Drug design

KW - Nitrogen heterocycles

KW - Structure-activity relationships

KW - β-secretase

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Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1

Abstract

Keywords

ASJC Scopus subject areas

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