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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Udgivet i:ACS Med Chem Lett
Main Authors: 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.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2019
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7003998/
https://ncbi.nlm.nih.gov/pubmed/32038769
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00345
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