title: New analogues of agmatine with higher affinity to imidazoline receptors.
abstract: Compilation of agmatine structure and imidazoline ring leads to a new family of imidazoline/alpha(2)-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. Constraining of the guanidine moiety into heterocyclic ring improved the affinities of the resultant fusion compounds in comparison to agmatine itself. In this work, the synthetic approach and results for I(1), I(2), and alpha(2)-adrenoceptors affinities are reported.
authors.affiliation: Department of Pharmaceutical Technology and Biochemistry, The Faculty of Chemistry, Gdańsk University of Technology, Narutowicza St. 11/12, 80-952 Gdańsk, Poland.
authors.forename: Adam P
authors.initials: AP
authors.lastname: Treder
authors.forename: Ryszard
authors.initials: R
authors.lastname: Andruszkiewicz
authors.forename: Włodzimierz
authors.initials: W
authors.lastname: Zgoda
authors.forename: Celeste
authors.initials: C
authors.lastname: Ford
authors.forename: Alan L
authors.initials: AL
authors.lastname: Hudson
mesh_terms: D000376:Agmatine / Q000031:analogs & derivatives* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003000:Clonidine / Q000494:pharmacology; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D019791:Guanidine / Q000737:chemistry; D006801:Humans; D007093:Imidazoles; D054755:Imidazoline Receptors / Q000737:chemistry* / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D011485:Protein Binding; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D011993:Recombinant Fusion Proteins / Q000737:chemistry
chemical_list: D007093:Imidazoles; D054755:Imidazoline Receptors; D018341:Receptors, Adrenergic, alpha-2; D011993:Recombinant Fusion Proteins; D000376:Agmatine; D019791:Guanidine; D003000:Clonidine