Further optimization of the M(1) PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

This letter describes the continued chemical optimization of the VU0453595 series of M(1) positive allosteric modulators (PAMs). By surveying alternative 5,6- and 6,6-heterobicylic cores for the 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one core of VU453595, we found new cores that engendered not only...

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Gepubliceerd in:Bioorg Med Chem Lett
Hoofdauteurs: Panarese, Joseph D., Cho, Hykeyung P., Adams, Jeffrey J., Nance, Kellie D., Garcia-Barrantes, Pedro M., Chang, Sichen, Morrison, Ryan D., Blobaum, Anna L., Niswender, Colleen M., Stauffer, Shaun R., Conn, P. Jeffrey, Lindsley, Craig W.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2016
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Article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5082649/
https://ncbi.nlm.nih.gov/pubmed/27173801
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.04.083
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