Download MendeleyPotent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Iserloh, U., Wu, Y., Cumming, J.N., Pan, J., Wang, L.Y., Stamford, A.W., Kennedy, M.E., Kuvelkar, R., Chen, X., Parker, E.M., Strickland, C., Voigt, J.(2008) Bioorg Med Chem Lett 18: 414-417
- PubMed: 18023580
- DOI: https://doi.org/10.1016/j.bmcl.2007.10.116
- Primary Citation of Related Structures:
2QK5, 2QMD, 2QMF, 2QP8 - PubMed Abstract:
Based on lead compound 1 identified from the patent literature, we developed novel patentable BACE-1 inhibitors by introducing a cyclic amine scaffold. Extensive SAR studies on both pyrrolidines and piperidines ultimately led to inhibitor 2f, one of the most potent inhibitors synthesized to date.
Organizational Affiliation:
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
