6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective α1A adrenoceptor partial agonists

Novel pyrroloimidazoles have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor subtypes. Pyrimidine 19 possessed attractive CNS drug-like properties with good membrane permeability and no evidence for P-gp mediated efflux.

Graphical abstractNovel pyrroloimidazoles have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor subtypes. Pyrimidine 20 possessed attractive CNS drug-like properties with good membrane permeability and no evidence for P-gp mediated efflux.Figure optionsDownload full-size imageDownload as PowerPoint slide