Challenges in the development of an M(4) PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

This letter describes the chemical optimization of a novel series of M(4) positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core, developed via iterative parallel synthesis, and culminating in the highly utilized rodent in vivo tool compound, VU0467154 (5). This is the...

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Udgivet i:Bioorg Med Chem Lett
Main Authors: Wood, Michael R., Noetzel, Meredith J., Poslusney, Michael S., Melancon, Bruce J., Tarr, James C., Lamsal, Atin, Chang, Sichen, Luscombe, Vincent B., Weiner, Rebecca L., Cho, Hyekyung P., Bubser, Michael, Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Engers, Darren W., Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Format: Artigo
Sprog:Inglês
Udgivet: 2016
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5340297/
https://ncbi.nlm.nih.gov/pubmed/27939174
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.11.086
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