Novel M(4) positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands

This letter describes a focused exercise to explore the role of the β-amino carboxamide moiety found in all of the first generation M(4) PAMs and question if the NH(2) group served solely to stabilize an intramolecular hydrogen bond (IMHB) and enforce planarity. To address this issue (and to potenti...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Poslusney, Michael S., Salovich, James M., Wood, Michael R., Melancon, Bruce J., Bollinger, Katrina A., Luscombe, Vincent B., Rodriguez, Alice L., Engers, Darren W., Bridges, Thomas M., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6690489/
https://ncbi.nlm.nih.gov/pubmed/30580918
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.12.039
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