Challenges in the development of an M(4) PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides

Herein we describe the continued optimization of M(4) positive allosteric modulators (PAMs) within the 5-amino-thieno[2,3-c]pyridazine series of compounds. In this letter, we disclose our studies on tertiary amides derived from substituted azetidines. This series provided excellent CNS penetration,...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Tarr, James C., Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Lamsal, Atin, Luscombe, Vincent B., Rodriguez, Alice L., Byers, Frank W., Chang, Sichen, Cho, Hyekyung P., Engers, Darren W., Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6542369/
https://ncbi.nlm.nih.gov/pubmed/29089231
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.10.053
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