Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481

[Image: see text] A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the bicyclic pyrimidine γ-secretase modulator BMS-932481. The compound showed robust reductions of Aβ(1–42) and Aβ(1–40) in the plas...

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Detalles Bibliográficos
Autores principales: Boy, Kenneth M., Guernon, Jason M., Zuev, Dmitry S., Xu, Li, Zhang, Yunhui, Shi, Jianliang, Marcin, Lawrence R., Higgins, Mendi A., Wu, Yong-Jin, Krishnananthan, Subramaniam, Li, Jianqing, Trehan, Ashok, Smith, Daniel, Toyn, Jeremy H., Meredith, Jere E., Burton, Catherine R., Kimura, S. Roy, Zvyaga, Tatyana, Zhuo, Xiaoliang, Lentz, Kimberley A., Grace, James E., Denton, Rex, Morrison, John S., Mathur, Arvind, Albright, Charles F., Ahlijanian, Michael K., Olson, Richard E., Thompson, Lorin A., Macor, John E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6421538/
https://www.ncbi.nlm.nih.gov/pubmed/30891132
http://dx.doi.org/10.1021/acsmedchemlett.8b00541

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