A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase
ACS Medicinal Chemistry Letters2012Vol. 3(11), pp. 886–891
Citations Over TimeTop 13% of 2012 papers
Matthew R. Kaller, Scott S. Harried, Brian K. Albrecht, Patricia Amarante, Safura Babu‐Khan, Michael D. Bartberger, James Brown, Ryan Brown, Kui Chen, Yuan Cheng, Martin Citron, Michael D. Croghan, Russell F. Graceffa, Dean Hickman, Ted Judd, Chuck Kriemen, Daniel S. La, Vivian Li, Patrícia Luciana da Costa Lopez, Yi Luo, C. E. Masse, Holger Monenschein, Thomas T. Nguyen, Lewis D. Pennington, Tisha San Miguel, E. Allen Sickmier, Robert C. Wahl, Matthew M. Weiss, Paul H. Wen, Toni Williamson, Stephen Wood, May Xue, Bryant H. Yang, Jianhua Zhang, Vinod F. Patel, Wenge Zhong, Stephen A. Hitchcock
Abstract
β-Secretase inhibitors are potentially disease-modifying treatments for Alzheimer's disease. Previous efforts in our laboratory have resulted in hydroxyethylamine-derived inhibitors such as 1 with low nanomolar potency against β-site amyloid precursor protein cleaving enzyme (BACE). When dosed intravenously, compound 1 was also shown to significantly reduce Aβ40 levels in plasma, brain, and cerebral spinal fluid. Herein, we report further optimizations that led to the discovery of inhibitor 16 as a novel, potent, and orally efficacious BACE inhibitor.
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