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Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

This letter describes the further chemical optimization of VU0424238 (auglurant), an mGlu(5) NAM clinical candidate that failed in non-human primate (NHP) 28 day toxicology due to accumulation of a species-specific aldehyde oxidase (AO) metabolite of the pyrimidine head group. Here, we excised the p...

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發表在:Bioorg Med Chem Lett
Main Authors: Felts, Andrew S., Bollinger, Katrina A., Brassard, Christopher J., Rodriguez, Alice L., Morrison, Ryan D., Daniels, J. Scott, Blobaum, Anna L., Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Emmitte, Kyle A., Lindsley, Craig W.
格式: Artigo
語言:Inglês
出版: 2018
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在線閱讀:https://ncbi.nlm.nih.gov/pmc/articles/PMC6295259/
https://ncbi.nlm.nih.gov/pubmed/30446311
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.11.017
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