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Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality

[Image: see text] A growing subset of β-secretase (BACE1) inhibitors for the treatment of Alzheimer’s disease (AD) utilizes an anilide chemotype that engages a key residue (Gly230) in the BACE1 binding site. Although the anilide moiety affords excellent potency, it simultaneously introduces a third...

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Detalles Bibliográficos
Autores principales: Butler, Christopher R., Ogilvie, Kevin, Martinez-Alsina, Luis, Barreiro, Gabriela, Beck, Elizabeth M., Nolan, Charles E., Atchison, Kevin, Benvenuti, Eric, Buzon, Leanne, Doran, Shawn, Gonzales, Cathleen, Helal, Christopher J., Hou, Xinjun, Hsu, Mei-Hui, Johnson, Eric F., Lapham, Kimberly, Lanyon, Lorraine, Parris, Kevin, O’Neill, Brian T., Riddell, David, Robshaw, Ashley, Vajdos, Felix, Brodney, Michael A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5461923/
https://www.ncbi.nlm.nih.gov/pubmed/27997172
http://dx.doi.org/10.1021/acs.jmedchem.6b01451