Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 1. SAR of modifications to the central aryl core

This letter describes the lead optimization of the VU0486321 series of mGlu(1) positive allosteric modulators (PAMs). While first generation PAMs from Roche were reported in the late 1990s, little effort has focused on the development of mGlu(1) PAMs since. New genetic data linking loss-of-function...

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Vydáno v:Bioorg Med Chem Lett
Hlavní autoři: Garcia-Barrantes, Pedro M., Cho, Hyekyung P., Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2015
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4758672/
https://ncbi.nlm.nih.gov/pubmed/26476971
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2015.10.013
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