Design and synthesis of bicyclic heterocycles as potent ¦Ã-secretase modulators
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- 作者：Daniel Oehlrich ; Frederik J.R. Rombouts ; Didier Berthelot ; Fran?ois P. Bischoff ; Michel A.J. De Cleyn ; Libuse Jaroskova ; Gregor Macdonald ; Marc Mercken ; Michel Surkyn ; Andr¨¦s A. Trabanco ; Gary Tresadern ; Sven Van Br ; t ; Adriana I. Velter ; Tongfei Wu ; Harrie J.M. Gijsen
- 关键词：Alzheimer&rsquo ; s disease ; ¦Ã-Secretase modulators
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：1 September, 2013
- 年：2013
- 卷：23
- 期：17
- 页码：4794-4800
- 全文大小：1475 K
文摘
The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a ¦Ã-secretase modulator is described. This is a potential disease modifying anti-Alzheimer¡¯s drug which demonstrated high in vitro and in vivo potency against A¦Â42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.