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...

תיאור מלא

שמור ב:
מידע ביבליוגרפי
הוצא לאור ב:Bioorg Med Chem Lett
Main Authors: 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.
פורמט: Artigo
שפה:Inglês
יצא לאור: 2016
נושאים:
Article
גישה מקוונת: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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