title: 2-[(Arylmethoxy)imino]imidazolidines with potential biological activities.
abstract: A series of 2-[(arylmethoxy)imino]imidazolidines was synthesized by reacting 2-chloro-4,5-dihydroimidazole with corresponding O-arylmethylhydroxylamines and evaluated for their alpha-, alpha2-adrenergic and imidazoline I1, I2 receptor binding affinities. The most potent 2-[(naphthalen-1-ylmethoxy)imino]imidazolidine showed a high selectivity and good affinity for the [3H]prazosin-labeled alpha1-adrenoceptors (K(i) = 107 nM). Representative compounds of this series were also tested in vivo for possible circulatory effects in rats after intravenous administration.
authors.affiliation: Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland. js@amg.gda.pl
authors.forename: Jarosław
authors.initials: J
authors.lastname: Saczewski
authors.forename: Alan L
authors.initials: AL
authors.lastname: Hudson
authors.forename: Apolonia
authors.initials: A
authors.lastname: Rybczyńska
mesh_terms: D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D048289:Imidazolidines / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D054755:Imidazoline Receptors / Q000378:metabolism; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D048289:Imidazolidines; D054755:Imidazoline Receptors; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; C410887:imidazoline I1 receptors; C487767:imidazoline receptor 2