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Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

This letter describes the further chemical optimization of the picolinamide-derived family of mGlu(4) PAMs wherein we identified a 3-amino substituent to the picolinamide warhead that engendered potency, CNS penetration and in vivo efficacy. From this optimization campaign, VU0477886 emerged as a po...

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Publicat a:Bioorg Med Chem Lett
Autors principals: Gogliotti, Rocco D., Engers, Darren W., Garcia-Barrantes, Pedro M., Panarese, Joseph D., Gentry, Patrick R., Blobaum, Anna L., Morrison, Ryan D., Daniels, J. Scott, Thompson, Analisa D., Jones, Carrie K., Conn, P. Jeffrey, Niswender, Colleen M., Lindsley, Craig W., Hopkins, Corey R.
Format: Artigo
Idioma:Inglês
Publicat: 2016
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC4899947/
https://ncbi.nlm.nih.gov/pubmed/27131990
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.04.041
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