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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Vydáno v:ACS Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2016
On-line přístup: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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