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 journalArticlepeer-review

29 Scopus citations


(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 languageEnglish (US)
Pages (from-to)995-999
Number of pages5
Issue number7
StatePublished - Jul 9 2007
Externally publishedYes


  • 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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