Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

This letter details the continued chemical optimization of a novel series of M(4) positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core by incorporating a 3-amino azetidine amide moiety. The analogs described within this work represent the most potent M(4) PAMs report...

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Publicado no:Bioorg Med Chem Lett
Main Authors: Tarr, James C., Wood, Michael R., Noetzel, Meredith J., Bertron, Jeanette, Weiner, Rebecca L., Rodriguez, Alice L., Lamsal, Atin, Byers, Frank W., Chang, Sichen, Cho, Hyekyung P., 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/PMC5518475/
https://ncbi.nlm.nih.gov/pubmed/28522253
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.05.014
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