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Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol O-Methyltransferase

[Image: see text] A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic nitrogen of the core scaffold gave the most potent inhibitors within this series. Rat pharmacokinetic studies showed medium to...

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Detalles Bibliográficos
Autores principales: Ernst, Glen, Akuma, Daniel, Au, Vinh, Buchler, Ingrid P., Byers, Spencer, Carr, Gregory V., Defays, Sabine, de León, Pablo, Demaude, Thierry, DePasquale, Michael, Durieu, Véronique, Huang, Yifang, Jigorel, Emilie, Kimos, Martha, Kolobova, Anna, Montel, Florian, Moureau, Florence, Poslusney, Michael, Swinnen, Dominique, Vandergeten, Marie-Christine, Van houtvin, Nathalie, Wei, Huijun, White, Noelle, Wood, Martyn, Barrow, James C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003998/
https://www.ncbi.nlm.nih.gov/pubmed/32038769
http://dx.doi.org/10.1021/acsmedchemlett.9b00345