Novel 2-imidazoles as potent and selective α1A adrenoceptor partial agonists

Novel 2-imidazoles have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor sub-types. Sulfonamide 23 possessed attractive drug-like properties with respect to physicochemical and ADME properties and wide ligand selectivity.

Graphical abstractA series of novel 2-imidazoles is described, which combine potent and selective α1A partial agonist pharmacology with good drug-like properties.Figure optionsDownload full-size imageDownload as PowerPoint slide