Potent and selective α1A adrenoceptor partial agonists—Novel imidazole frameworks

Novel imidazole frameworks have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity.

Graphical abstractNovel imidazole frameworks have been identified as potent and selective α1A partial agonists with good CNS drug-like properties.Figure optionsDownload full-size imageDownload as PowerPoint slide