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Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2. SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool

This letter describes the further lead optimization of the VU0486321 series of mGlu(1) positive allosteric modulators (PAMs), driven by recent genetic data linking loss of function GRM1 to schizophrenia. Steep and caveat-laden SAR plagues the series, but ultimately potent mGlu(1) PAMs (EC(50)s ~ 5 n...

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Bibliografiske detaljer
Udgivet i:Bioorg Med Chem Lett
Main Authors: Garcia-Barrantes, Pedro M., Cho, Hyekyung P., Metts, Adam M., Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Format: Artigo
Sprog:Inglês
Udgivet: 2016
Fag:
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4794757/
https://ncbi.nlm.nih.gov/pubmed/26778256
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.12.104
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