摘要
From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived A尾 following oral administration to rats. Herein we report SAR development in the S3 and F鈥?subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound.