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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 4
BKCSDE 32(4)
April 20, 2011 

Synthesis and Biological Activities of (4-Arylpiperazinyl)piperidines as Nonpeptide BACE 1 Inhibitors
Poojary Boja, SunWoo Won, Dong Hoon Suh, Jeonghyun Chu, Woo Kyu Park, Hee Jong Lim *
Alzheimer’s Disease (AD), BACE 1 (β-secretase), Non-peptidomimetic inhibitors, Arylpiperazinylpiperidines
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.
1249 - 1252
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