Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists

[Image: see text] We describe the synthesis and SAR of 1,2,3-triazolopiperidines as a novel series of potent, brain penetrant P2X7 antagonists. Initial efforts yielded a series of potent human P2X7R antagonists with moderate to weak rodent potency, some CYP inhibition, poor metabolic stability, and...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Savall, Brad M., Wu, Duncan, De Angelis, Meri, Carruthers, Nicholas I., Ao, Hong, Wang, Qi, Lord, Brian, Bhattacharya, Anindya, Letavic, Michael A.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4468405/
https://ncbi.nlm.nih.gov/pubmed/26101572
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00089
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