1304134-79-9Relevant articles and documents
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
Oehlrich, Daniel,Rombouts, Frederik J.R.,Berthelot, Didier,Bischoff, Francois P.,De Cleyn, Michel A.J.,Jaroskova, Libuse,MacDonald, Gregor,Mercken, Marc,Surkyn, Michel,Trabanco, Andres A.,Tresadern, Gary,Van Brandt, Sven,Velter, Adriana I.,Wu, Tongfei,Gijsen, Harrie J.M.
, p. 4794 - 4800 (2013/09/02)
The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a γ-secretase modulator is described. This is a potential disease modifying anti-Alzheimer's drug which demonstrated high in vitro and in vivo potency against Aβ42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
