Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Novel 2-imidazoles have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Sulfonamide 23 possessed attractive drug-like properties with respect to physicochemical and ADME properties and wide ligand selectivity.
Whitlock
Gavin A
GA
Department of Chemistry, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. gavin.whitlock@pfizer.com
Conlon
Kelly
K
McMurray
Gordon
G
Roberts
Lee R
LR
Stobie
Alan
A
Thurlow
Richard J
RJ
D058646:Adrenergic alpha-1 Receptor Agonists; D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000138:chemical synthesis / Q000627:therapeutic use*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000627:therapeutic use*; D008956:Models, Chemical; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D014549:Urinary Incontinence / Q000188:drug therapy*
C547713:ADRA1A protein, human; C547716:ADRA1B protein, human; C547719:ADRA1D protein, human; C547768:ADRA2A protein, human; D058646:Adrenergic alpha-1 Receptor Agonists; D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; D013449:Sulfonamides