2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
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.
Speake
Jason D
JD
GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. jason.d.speake@gsk.com
Navas
Frank
F
Bishop
Michael J
MJ
Garrison
Deanna T
DT
Bigham
Eric C
EC
Hodson
Stephen J
SJ
Saussy
David L
DL
Liacos
Jim A
JA
Irving
Paul E
PE
Sherman
Bryan W
BW
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
D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D011720:Pyrazoles; D011758:Pyrroles; D014230:Triazoles