Design and synthesis of bicyclic heterocycles as potent I3-secretase modulators

The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a I3-secretase modulator is described. This is a potential disease modifying anti-Alzheimeras drug which demonstrated high in vitro and in vivo potency against AI242 peptide, reduced lipophilicity and enha...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-09, Vol.23 (17), p.4794-4800
Main Authors: Oehlrich, Daniel, Rombouts, Frederik, Berthelot, Didier, Bischoff, Francois, Cleyn, Michel, Jaroskova, Libuse, Macdonald, Gregor, Mercken, Marc, Surkyn, Michel, Trabanco, Andres, Tresadern, Gary, Brandt, Sven, Velter, Adriana, Wu, Tongfei, Gijsen, Harrie
Format: Article
Language:English
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Summary:The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a I3-secretase modulator is described. This is a potential disease modifying anti-Alzheimeras drug which demonstrated high in vitro and in vivo potency against AI242 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.06.100