Optimization of an ether series of mGlu(5) positive allosteric modulators: Molecular determinants of MPEP-site interaction crossover

We report the optimization of a series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on a simple acyclic ether series. Modifications led to a gain of MPEP site interaction through incorporation of a chiral amide in conjunction with a nicotin...

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Detalhes bibliográficos
Main Authors: Manka, Jason T., Vinson, Paige N., Gregory, Karen J., Zhou, Ya, Williams, Richard, Gogi, Kiran, Days, Emily, Jadhav, Satya, Herman, Elizabeth J., Lavreysen, Hilde, Mackie, Claire, Bartolomé, José M., Macdonald, Gregor J., Steckler, Thomas, Daniels, J. Scott, Weaver, C. David, Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3755010/
https://ncbi.nlm.nih.gov/pubmed/22981332
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.08.043
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