Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent IKur Inhibitor
2016
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 channelselective inhibitor with robust efficacy in the preclinical rat ventricular
effective refractory period(VERP) model and the rabbit atrial
effective refractory period(AERP) model.
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