Discovery of Molecular Switches within the ADX-47273 mGlu(5) PAM scaffold that modulate modes of pharmacology to afford potent mGlu(5) NAMs, PAMs and partial antagonists

This Letter describes a chemical lead optimization campaign directed at a weak mGlu(5) NAM discovered while developing SAR for the mGlu(5) PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu(5) NAMs, mGlu(5) PAMs as well as mG...

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Hauptverfasser: Lamb, Jeffrey P., Engers, Darren W., Niswender, Colleen M., Rodriguez, Alice L., Venable, Daryl F., Conn, P. Jeffrey, Lindsley, Craig W.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2010
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3179182/
https://ncbi.nlm.nih.gov/pubmed/21183344
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2010.11.119
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