| Literature DB >> 27660686 |
Heather J Finlay1, James A Johnson1, John L Lloyd1, Ji Jiang1, James Neels1, Prashantha Gunaga2, Abhisek Banerjee2, Naveen Dhondi2, Anjaneya Chimalakonda1, Sandhya Mandlekar2, Mary Lee Conder1, Harinath Sale2, Dezhi Xing1, Paul Levesque1, Ruth R Wexler1.
Abstract
A new series of phenylquinazoline inhibitors of Kv 1.5 is disclosed. The series was optimized for Kv 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 identified as a potent and ion channel selective inhibitor with robust efficacy in the preclinical rat ventricular effective refractory period (VERP) model and the rabbit atrial effective refractory period (AERP) model.Entities:
Keywords: Kv 1.5; atrial effective refractory period; phenylquinazoline; ventricular effective refractory period
Year: 2016 PMID： 27660686 PMCID： PMC5018869 DOI： 10.1021/acsmedchemlett.6b00117
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345