Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators
…, MAJ De Cleyn, L Jaroskova, G Macdonald…
Index: 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. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 17 p. 4794 - 4800
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Citation Number: 10
Abstract
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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