1398519-75-9Relevant academic research and scientific papers
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and cns penetrable BACE inhibitors for the treatment of alzheimers disease
Huang, Hongbing,La, Daniel S.,Cheng, Alan C.,Whittington, Douglas A.,Patel, Vinod F.,Chen, Kui,Dineen, Thomas A.,Epstein, Oleg,Graceffa, Russell,Hickman, Dean,Kiang,Louie, Steven,Luo, Yi,Wahl, Robert C.,Wen, Paul H.,Wood, Stephen,Fremeau, Robert T.
, p. 9156 - 9169 (2012)
A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the structurally related aspartyl protease cathepsin D. Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound 11a resulted in a significant reduction of CNS Aβ40 in naive rats.
