Chen, Jian Jeffrey; Liu, Qingyian; Yuan, Chester; Gore, Vijay; Lopez, Patricia; Ma, Vu; Amegadzie, Albert; Qian, Wenyuan; Judd, Ted C.; Minatti, Ana E.; Brown, James; Cheng, Yuan; Xue, May; Zhong, Wenge; Dineen, Thomas A.; Epstein, Oleg; Human, Jason; Kreiman, Charles; Marx, Isaac; Weiss, Matthew M.; Hitchcock, Stephen A.; Powers, Timothy S.; Chen, Kui; Wen, Paul H.; Whittington, Douglas A.; Cheng, Alan C.; Bartberger, Michael D.; Hickman, Dean; Werner, Jonathan A.; Vargas, Hugo M.; Everds, Nancy E.; Vonderfecht, Steven L.; Dunn, Robert T. II; Wood, Stephen; Fremeau, Robert T. Jr.; White, Ryan D.; Patel, Vinod F. published the artcile< Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease>, Computed Properties of 660867-80-1, the main research area is aminooxazoline azaxanthene derivative preparation oral beta secretase inhibitor Alzheimer’s; 3-Azaxanthene; Alzheimer’s disease (AD); Aminooxazoline; Amyloid; Aβ peptides; Xanthene; β-Secretase (BACE1).
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model.
Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Computed Properties of 660867-80-1.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts