Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

This letter describes the further lead optimization of the VU0486321 series of mGlu(1) positive allosteric modulators (PAMs), focused on addressing the recurrent issue of plasma instability of the phthalimide moiety. Here, we evaluated a number of phthalimide bioisosteres, and ultimately identified...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Garcia-Barrantes, Pedro M., Cho, Hyekyung P., Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, 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/PMC4823774/
https://ncbi.nlm.nih.gov/pubmed/26988302
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.03.031
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