The discovery of VU0486846: steep SAR from a series of M(1) PAMs based on a novel benzomorpholine core

This letter describes the chemical optimization of a new series of M(1) positive allosteric modulators (PAMs) based on a novel benzomorpholine core, developed via iterative parallel synthesis, and culminating in the highly utilized rodent in vivo tool compound, VU0486846 (7), devoid of adverse effec...

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Bibliografski detalji
Izdano u:Bioorg Med Chem Lett
Glavni autori: Bertron, Jeanette L., Cho, Hyekyung P., Garcia-Barrantes, Pedro M., Panarese, Joseph D., Salovich, James M., Nance, Kellie D., Engers, Darren W., Rook, Jerri M., Blobaum, Anna L., Niswender, Colleen M., Stauffer, Shaun R., Conn, P. Jeffrey, Lindsley, Craig W.
Format: Artigo
Jezik:Inglês
Izdano: 2018
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Article
Online pristup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6427922/
https://ncbi.nlm.nih.gov/pubmed/29754948
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.05.009
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