New analogues of agmatine with higher affinity to imidazoline receptors.
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.
Treder
Adam P
AP
Department of Pharmaceutical Technology and Biochemistry, The Faculty of Chemistry, Gdańsk University of Technology, Narutowicza St. 11/12, 80-952 Gdańsk, Poland.
Andruszkiewicz
Ryszard
R
Zgoda
Włodzimierz
W
Ford
Celeste
C
Hudson
Alan L
AL
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
D007093:Imidazoles; D054755:Imidazoline Receptors; D018341:Receptors, Adrenergic, alpha-2; D011993:Recombinant Fusion Proteins; D000376:Agmatine; D019791:Guanidine; D003000:Clonidine