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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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| Publié dans: | Bioorg Med Chem Lett |
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| Auteurs principaux: | , , , , , , |
| Format: | Artigo |
| Langue: | Inglês |
| Publié: |
2016
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| Sujets: | |
| Accès en ligne: | 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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