Bulletin of the Korean Chemical Society

  • 제32권4호
  • /
  • Pages.1249-1252
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  • 2011
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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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)
  • 투고 : 2010.12.28
  • 심사 : 2011.02.14
  • 발행 : 2011.04.20
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초록

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.

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참고문헌

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  4. ][1,3]oxazine (PA-824) vol.58, pp.7, 2015, https://doi.org/10.1021/jm501608q
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