Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Biological Activities of (4-Arylpiperazinyl)piperidines as Nonpeptide BACE 1 Inhibitors

  • Boja, Poojary (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Won, Sun-Woo (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Suh, Dong-Hoon (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Chu, Jeong-Hyun (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Park, Woo-Kyu (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Lim, Hee-Jong (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)
  • Received : 2010.12.28
  • Accepted : 2011.02.14
  • Published : 2011.04.20
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Abstract

Inhibition of BACE 1 activity is considered as a promising therapeutic target for Alzheimer's Disease (AD). Synthesis and inhibitory activities of (4-arylpiperazinyl)piperidines by bioisosteric replacement of a biaryl group with an arylpiperazine as BACE 1 inhibitors are described. The resulting (4-arylpiperazinyl)piperidines represent novel nonpeptide BACE 1 inhibitors with improved in vitro potency.

Keywords

References

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