Synthesis and structure–activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists

A series of 8-azabicyclo[3.2.1]octane amine hNK1 antagonists has been investigated and structure–activity relationships of the benzylamine and 6-exo substituents described. Acidic substituents at C6 give a series of high affinity compounds for hNK1 with selectivity over the hERG channel.

Graphical abstractA series of 8-azabicyclo[3.2.1]octane benzylamine hNK1 antagonists has been explored. Substitution with acidic moieties at the 6-exo position leads to high affinity hNK1 antagonists which are selective over the hERG channel.Figure optionsDownload full-size imageDownload as PowerPoint slide