Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides

…, K Kolmodin, S Karlström, S von Berg…

文献索引：Berg, Stefan; Swahn, Britt-Marie; Kolmodin, Karin; Karlstroem, Sofia; Von Berg, Stefan; Soederman, Peter; Holenz, Joerg; Lindstroem, Johan; Sundstroem, Marie; Turek, Dominika; Kihlstroem, Jacob; Slivo, Can; Andersson, Lars; Pyring, David; Rotticci, Didier; Oehberg, Liselotte; Kers, Annika; Bogar, Krisztian; Von Kieseritzky, Fredrik; Bergh, Margareta; Eketjaell, Susanna; Georgievska, Biljana; Jeppsson, Fredrik; Faelting, Johanna; Janson, Juliette; Olsson, Lise-Lotte Journal of Medicinal Chemistry, 2012 , vol. 55, # 21 p. 9346 - 9361,16

全文：HTML全文

被引用次数: 45

摘要

The evaluation of a series of aminoisoindoles as β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors and the discovery of a clinical candidate drug for Alzheimer's disease,(S)-32 (AZD3839), are described. The improvement in permeability properties by the introduction of fluorine adjacent to the amidine moiety, resulting in in vivo brain reduction of Aβ40, is discussed. Due to the basic nature of these compounds, they displayed affinity ...