[4-(Phenoxy)pyridin-3-yl]methylamines: A new class of selective noradrenaline reuptake inhibitors

[4-(Phenoxy)pyridine-3-yl]methylamines are disclosed as a new series of selective noradrenaline reuptake inhibitors (NRI). Structure–activity relationships established that potent NRI activity could be achieved by appropriate substitution at the 2-position of the phenoxy ring. Compound 31 demonstrated potent NRI activity combined with good selectivity over serotonin and dopamine reuptake and no significant off-target pharmacology.

Graphical abstractPyridinyl phenyl ethers are disclosed as a new series of selective noradrenaline reuptake inhibitors (NRI). Structure–activity relationships established that potent NRI activity could be achieved by appropriate substitution at the 2-position of the phenoxy ring. Compound 31 demonstrated potent NRI activity combined with good selectivity over serotonin and dopamine reuptake, and no significant off-target pharmacology.Figure optionsDownload full-size imageDownload as PowerPoint slide