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Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
1Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jared.cumming@spcorp.com
Bioorganic & Medicinal Chemistry Letters
|May 13, 2008
Abstract:
Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' pocket.

