1373754-45-0Relevant academic research and scientific papers
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid
Weiss, Matthew M.,Williamson, Toni,Babu-Khan, Safura,Bartberger, Michael D.,Brown, James,Chen, Kui,Cheng, Yuan,Citron, Martin,Croghan, Michael D.,Dineen, Thomas A.,Esmay, Joel,Graceffa, Russell F.,Harried, Scott S.,Hickman, Dean,Hitchcock, Stephen A.,Horne, Daniel B.,Huang, Hongbing,Imbeah-Ampiah, Ronke,Judd, Ted,Kaller, Matthew R.,Kreiman, Charles R.,La, Daniel S.,Li, Vivian,Lopez, Patricia,Louie, Steven,Monenschein, Holger,Nguyen, Thomas T.,Pennington, Lewis D.,Rattan, Claire,San Miguel, Tisha,Sickmier, E.Allen,Wahl, Robert C.,Wen, Paul H.,Wood, Stephen,Xue, Qiufen,Yang, Bryant H.,Patel, Vinod F.,Zhong, Wenge
, p. 9009 - 9024 (2013/01/15)
A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and poor CNS partitioning. This work identified a series of benzodioxolane analogues that possessed improved metabolic stability and increased oral bioavailability. Subsequent efforts focused on improving CNS exposure by limiting susceptibility to Pgp-mediated efflux and identified an inhibitor which demonstrated robust and sustained reduction of CNS β-amyloid (Aβ) in Sprague-Dawley rats following oral administration.
