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http://dx.doi.org/10.5012/bkcs.2011.32.4.1249

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)
Publication Information
Bulletin of the Korean Chemical Society / v.32, no.4, 2011 , pp. 1249-1252 More about this Journal
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
Alzheimer's Disease (AD); BACE 1 (${\beta}$-secretase); Non-peptidomimetic inhibitors; Arylpiperazinylpiperidines;
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