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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發表在: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.
格式: Artigo
語言:Inglês
出版: American Chemical Society 2016
在線閱讀: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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