1. Anilinotriazoles as potent gamma secretase modulators.
- Author
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Velter AI, Bischoff FP, Berthelot D, De Cleyn M, Oehlrich D, Jaroskova L, Macdonald G, Minne G, Pieters S, Rombouts F, Van Brandt S, Van Roosbroeck Y, Surkyn M, Trabanco AA, Tresadern G, Wu T, Borghys H, Mercken M, Masungi C, and Gijsen H more...
- Subjects
- Amyloid Precursor Protein Secretases metabolism, Amyloid beta-Peptides chemistry, Amyloid beta-Peptides metabolism, Aniline Compounds chemical synthesis, Aniline Compounds metabolism, Animals, Brain metabolism, Drug Design, Humans, Mice, Mice, Transgenic, Protein Binding, Structure-Activity Relationship, Triazoles chemical synthesis, Triazoles metabolism, Amyloid Precursor Protein Secretases antagonists & inhibitors, Aniline Compounds chemistry, Triazoles chemistry
- Abstract
The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in vivo potency with an acceptable drug-like profile., (Copyright © 2014 Elsevier Ltd. All rights reserved.) more...
- Published
- 2014
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