Development of 2-aminooxazoline 3-azaxanthene β-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D

As part of an ongoing effort at Amgen to develop a disease-modifying therapy for Alzheimer's disease, we have previously used the aminooxazoline xanthene (AOX) scaffold to generate potent and orally efficacious BACE1 inhibitors. While AOX-BACE1 inhibitors demonstrated acceptable cardiovascular...

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Detalhes bibliográficos
Publicado no:Medchemcomm
Main Authors: Low, Jonathan D., Bartberger, Michael D., Chen, Kui, Cheng, Yuan, Fielden, Mark R., Gore, Vijay, Hickman, Dean, Liu, Qingyian, Allen Sickmier, E., Vargas, Hugo M., Werner, Jonathan, White, Ryan D., Whittington, Douglas A., Wood, Stephen, Minatti, Ana E.
Formato: Artigo
Idioma:Inglês
Publicado em: Royal Society of Chemistry 2017
Assuntos:
Chemistry
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6072065/
https://ncbi.nlm.nih.gov/pubmed/30108829
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c7md00106a
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