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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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| Publicado no: | Bioorg Med Chem Lett |
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| Main Authors: | , , , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
2016
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| Assuntos: | |
| Acesso em linha: | 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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