Synthesis and biological activities of (4-arylpiperazinyl)piperidines as nonpeptide BACE 1 inhibitors

Bulletin of the Korean Chemical Society

Volumn 32, Issue 4, 2011, Pages 1249-1252

  Boja, Poojary ^a   Won, Sunwoo ^a   Suh, Dong Hoon ^a   Chu, Jeonghyun ^a   Park, Woo Kyu ^a   Lim, Hee Jong ^a  

^a Korea Research Institute of Chemical Technology   (South Korea)

Author keywords

Alzheimer's Disease (AD); Arylpiperazinylpiperidines; BACE 1 ( secretase); Non peptidomimetic inhibitors

Indexed keywords

ALZHEIMER'S DISEASE; ARYLPIPERAZINYLPIPERIDINES; BIOLOGICAL ACTIVITIES; IN-VITRO; INHIBITORY ACTIVITY; NONPEPTIDE; PEPTIDOMIMETICS; THERAPEUTIC TARGETS;

NEURODEGENERATIVE DISEASES;

EID: 79954570437     PISSN: 02532964     EISSN: 12295949     Source Type: Journal    
DOI: 10.5012/bkcs.2011.32.4.1249     Document Type: Article

References (18)

1. Mount, C.; Downton, C. Nat. Med. 2006, 12, 780.
2. (a) Shawn, J. S. Drug Dev. Res. 2009, 70, 101.
3. (b) Selkoe, D. J. Nature 1999, 399, A23.
4. Sinha, S.; Lieberburg, I. Proc. Natl. Acad. Sci. U.S.A. 1999, 96, 11049.
5. Hsiao, K.; Chapman, P.; Nilsen, S.; Eckman, C.; Harigaya, Y.; Younkin, S.; Yang, F.; Cole, G. Science 1996, 274, 99.
6. Luo, Y.; Bolon, B.; Damore, M. A.; Fitzpatrick, D.; Liu, H.; Zhang, J.; Yan, Q.; Vassar, R.; Citron, M. Neurobiol. Dis. 2003, 14, 81.
7. (a) Malamas, M. S.; Erdei, J.; Gunawan, I.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Jacobsen, S.; Magolda, R. L.; Pangalos, M.; Robichaud, A. J. Med. Chem. 2010, 53, 1146.
8. (b) Citron, M. Nature Rev. Neurosci. 2004, 5, 677.
9. (a) Gosh, A. K.; Shin, D. W.; Downs, D.; Koelsch, G.; Lin, X.; Ermolieff, J.; Tnag, J. J. Am. Chem. Soc. 2000, 122, 3522.
10. (b) Hanessian, S.; Yun, H.; Hou, Y.; Yang, G.; Bayrakdarian, M.; Therrien, E.; Moitessier, N.; Roggo, S.; Veenstra, S.; et al. J. Med. Chem. 2005, 48, 5175.
11. (c) Yang, W.; Lu, W.; Lu, Y.; Zhong, M.; Sun, J.; Thomas, A. E.; Wilkinson, J. M.; Fucini, R. V.; Lam, M.; Randal, M.; Shi, X.-P.; Jacobs, J. W.; McDowell, R. S.; Gordon, E. M.; Ballinger, M. D. J. Med. Chem. 2006, 49, 839.
12. (a) Edwards, P. D.; Albert, J. S.; Sylvester, M.; Aharony, D.; Andisik, D.; Callaghan, O.; Campbell, J. B.; Carr, R. A.; Chessari, G.; Congreve, M.; Frederickson, M.; Folmer, R. H.; Geschwindner, S.; Koether, G.; Kolmodin, K.; Krumrine, J.; Mauger, R. C.; Murray, C. W.; Olsson, L.-L.; Patel, S.; Spear, N.; Tian, G. J. Med. Chem. 2006, 49, 6158.
13. (b) Cole, D. C.; Manas, E. S.; Stock, J. R.; Condon, J. S.; Jennings, L. D.; Aulabaugh, A.; Chopra, R.; Cowling, R.; Ellingboe, J. W.; Fan, K. Y.; Harrison, B. L.; Hu, Y.; Jacobsen, S.; Jin, G.; Lin, L.; Lovering, F. E.; Malamas, M. S.; Stahl, M. L.; Strand, J.; Sukhdeo, M. N.; Svenson, K.; Turner, M. J.; Wagner, E.; Wu, J.; Zhou, P.; Bard, J. J. Med. Chem. 2007, 50, 5912.
14. (c) Malamas, M. S.; Erdei, J.; Gunawan, I.; Barnes, K.; Johnson, M.; Hui, Y.; Turner, J.; Hu, Y.; Erik Wagner, E.; Fan, K.; Olland, A.; Bard, J.; Robichaud, A. J. J. Med. Chem. 2009, 52, 6314.
15. Lim, H.-J.; Jung, M. H.; Choi, I. Y.; Park, W. K. Bull. Korean Chem. Soc. 2006, 27, 1371.
16. Zhang, A.; Neumeyer, J. L.; Baldessarini, R. J. Chem. Rev. 2007, 107, 274.
17. Boja, P.; Lim, H.-J. Z. Naturforsch. 2010, 65b, 197.
18. Huang, D.; Luthi, U.; Kolb, P.; Edler, K.; Cecchini, M.; Audetat, S.; Barberis, A.; Caflisch, A. J. Med. Chem. 2005, 48, 5108.