Potent pyrrolidine- and piperidine-based BACE-1 inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
- Schering-Plough
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. The discovery and development of novel BACE-1 inhibitors incorporating a cyclic amine scaffold is described.
- Research Organization:
- Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1006759
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (1) ; 01, 2008 Vol. 18; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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