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Title: Potent pyrrolidine- and piperidine-based BACE-1 inhibitors

Journal Article · · Bioorg. Med. Chem. Lett.

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:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
USDOE
OSTI ID:
1006759
Journal Information:
Bioorg. Med. Chem. Lett., Vol. 18, Issue (1) ; 01, 2008; ISSN 0960-894X
Country of Publication:
United States
Language:
ENGLISH