2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
A series of 2'-heteroaryl and 2'-oxime anilinomethylimidazolines was prepared and evaluated in in vitro functional assays for cloned human alpha1A, alpha1B, and alpha1D receptor subtypes. Potent and selective alpha1A agonists have been identified in these series.
Navas
Frank
F
Division of Chemistry, GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. fn28689@gsk.com
Bishop
Michael J
MJ
Garrison
Deanna T
DT
Hodson
Stephen J
SJ
Speake
Jason D
JD
Bigham
Eric C
EC
Drewry
David H
DH
Saussy
David L
DL
Liacos
James H
JH
Irving
Paul E
PE
Gobel
M Jeffrey
MJ
D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D020013:Calcium Signaling / Q000187:drug effects; D002460:Cell Line; D003001:Cloning, Molecular; D006571:Heterocyclic Compounds; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010091:Oximes; D010656:Phenylephrine / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism
C547713:ADRA1A protein, human; C547716:ADRA1B protein, human; C547719:ADRA1D protein, human; D058646:Adrenergic alpha-1 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D006571:Heterocyclic Compounds; D007093:Imidazoles; D010091:Oximes; D018340:Receptors, Adrenergic, alpha-1; D010656:Phenylephrine