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 Graham, Steven M. Pitzenberger, Georgia B. McGaughey, Dennis Colussi, Ming‐Tain Lai, Qian Huang,

ChemMedChem · 2007 · 39 citations · 12 references

Concepts

Abstract

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.

References

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