1373344-80-9Relevant academic research and scientific papers
Discovery of SCH 900229, a potent presenilin 1 selective γ-secretase inhibitor for the treatment of Alzheimer's disease
Wu, Wen-Lian,Domalski, Martin,Burnett, Duane A.,Josien, Hubert,Bara, Thomas,Rajagopalan, Murali,Xu, Ruo,Clader, John,Greenlee, William J.,Brunskill, Andrew,Hyde, Lynn A.,Del Vecchio, Robert A.,Cohen-Williams, Mary E.,Song, Lixin,Lee, Julie,Terracina, Giuseppe,Zhang, Qi,Nomeir, Amin,Parker, Eric M.,Zhang, Lili
, p. 892 - 896 (2013/01/15)
An exploration of the SAR of the side chain of a novel tricyclic series of γ-secretase inhibitors led to the identification of compound (-)-16 (SCH 900229), which is a potent and PS1 selective inhibitor of γ-secretase (Aβ40 IC50 = 1.3 nM). Compound (-)-16 demonstrated excellent lowering of Aβ after oral administration in preclinical animal models and was advanced to human clinical trials for further development as a therapeutic agent for the treatment of Alzheimer's disease.
