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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Vydáno v:Bioorg Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2016
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On-line přístup: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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