title: 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
abstract: The structure-activity relationship of 2'-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as alpha(1) adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent alpha(1A) subtype selective agonists have been identified.
authors.affiliation: GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. jason.d.speake@gsk.com
authors.forename: Jason D
authors.initials: JD
authors.lastname: Speake
authors.forename: Frank
authors.initials: F
authors.lastname: Navas
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bishop
authors.forename: Deanna T
authors.initials: DT
authors.lastname: Garrison
authors.forename: Eric C
authors.initials: EC
authors.lastname: Bigham
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Hodson
authors.forename: David L
authors.initials: DL
authors.lastname: Saussy
authors.forename: Jim A
authors.initials: JA
authors.lastname: Liacos
authors.forename: Paul E
authors.initials: PE
authors.lastname: Irving
authors.forename: Bryan W
authors.initials: BW
authors.lastname: Sherman
mesh_terms: D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D011720:Pyrazoles; D011758:Pyrroles; D014230:Triazoles