Discovery and SAR of a novel series of potent, CNS penetrant M(4) PAMs based on a non-enolizable ketone core: Challenges in disposition

This letter describes the chemical optimization of a novel series of M(4) PAMs based on a non-enolizable ketone core, identified from an MLPCN functional high-throughput screen. The HTS hit was potent, selective and CNS penetrant; however, the compound was highly cleared in vitro and in vivo. SAR pr...

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Опубликовано в: :Bioorg Med Chem Lett
Главные авторы: Wood, Michael R., Noetzel, Meredith J., Tarr, James C., Rodriguez, Alice L., Lamsal, Atin, Chang, Sichen, Foster, Jarrett J., Smith, Emery, Chase, Peter, Hodder, Peter S., Engers, Darren W., Niswender, Colleen M., Brandon, Nicholas J., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Формат: Artigo
Язык:Inglês
Опубликовано: 2016
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Article
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC4987221/
https://ncbi.nlm.nih.gov/pubmed/27476142
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.07.042
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