Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I(Kur) Inhibitor

[Image: see text] A new series of phenylquinazoline inhibitors of K(v) 1.5 is disclosed. The series was optimized for K(v) 1.5 potency, selectivity versus hERG, pharmacokinetic exposure, and pharmacodynamic potency. 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (13k) was ident...

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Udgivet i:ACS Med Chem Lett
Main Authors: Finlay, Heather J., Johnson, James A., Lloyd, John L., Jiang, Ji, Neels, James, Gunaga, Prashantha, Banerjee, Abhisek, Dhondi, Naveen, Chimalakonda, Anjaneya, Mandlekar, Sandhya, Conder, Mary Lee, Sale, Harinath, Xing, Dezhi, Levesque, Paul, Wexler, Ruth R.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2016
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5018869/
https://ncbi.nlm.nih.gov/pubmed/27660686
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00117
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