| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10595385 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
Abstract
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.
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Authors
Daniel Oehlrich, Frederik J.R. Rombouts, Didier Berthelot, François P. Bischoff, Michel A.J. De Cleyn, Libuse Jaroskova, Gregor Macdonald, Marc Mercken, Michel Surkyn, Andrés A. Trabanco, Gary Tresadern, Sven Van Brandt, Adriana I. Velter, Tongfei Wu,