双环分子
化学
亲脂性
哌啶
立体化学
体内
体外
肽
化学合成
酰胺
组合化学
生物化学
生物
生物技术
作者
Daniel Oehlrich,Frederik J. R. Rombouts,Didier Berthelot,François Paul Bischoff,Michel Anna Jozef De Cleyn,Libuse Jaroskova,Gregor James Macdonald,Marc Mercken,Michel Surkyn,Andrés A. Trabanco,Gary Tresadern,Sven Franciscus Anna Van Brandt,Adriana Ingrid Velter,Tongfei Wu,Harrie J.M. Gijsen
标识
DOI:10.1016/j.bmcl.2013.06.100
摘要
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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