Discovery and optimization of a novel series of highly CNS penetrant M(4) PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d] pyrimidine core

This Letter describes the chemical optimization of a novel series of M(4) positive allosteric modulators (PAMs) based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core, identified from an MLPCN functional high-throughput screen. The HTS hit was potent and selective, but not CNS penetr...

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Publicado no:Bioorg Med Chem Lett
Main Authors: Wood, Michael R., Noetzel, Meredith J., Engers, Julie L., Bollinger, Katrina A., Melancon, Bruce J., Tarr, James C., Han, Changho, West, Mary, Gregro, Alison R., Lamsal, Atin, Chang, Sichen, Ajmera, Sonia, Smith, Emery, Chase, Peter, Hodder, Peter S., Bubser, Michael, Jones, Carrie K., Hopkins, Corey R., Emmitte, Kyle A., Niswender, Colleen M., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4955361/
https://ncbi.nlm.nih.gov/pubmed/27185330
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.05.010
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