title: Synthesis, structure-activity relationship of some new anti-arrhythmic 5-arylidene imidazolidine-2,4-dione derivatives.
abstract: The synthesis of unsubstituted and halogen substituted 5-arylidene basic amide derivatives of imidazolidine-2,4-dione is described. Structural elucidation based on X-ray analysis was performed for four representative compounds. The effect of the studied compounds on the electrocardiogram was examined in vitro in the non-working heart perfusion test and that of an anti-arrhythmic activity in the rat coronary artery ligation-reperfusion model. The most active compound: (5Z)-(3-chloro)benzylidene-3-{2-[4-(hydroxyethyl)piperazin-1-yl]-2-oxoethyl}imidazolidine-2,4-dione has shown properties of the compounds belonging to class Ia, according to the Vaughan Williams classification. Chosen compounds evaluated in vivo were devoid of anticonvulsant and neurotoxical activity.
authors.affiliation: Department of Chemical Technology and Biotechnology of Drugs, Jagiellonian University Medical College, ul. Medyczna 9, 30-688 Kraków, Poland.
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Pekala
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Stadnicka
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Broda
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Zygmunt
authors.forename: Barbara
authors.initials: B
authors.lastname: Filipek
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kieć-Kononowicz
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000927:Anticonvulsants / Q000737:chemistry; D001145:Arrhythmias, Cardiac / Q000188:drug therapy* / Q000209:etiology; D018360:Crystallography, X-Ray; D006321:Heart / Q000187:drug effects; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D015425:Myocardial Reperfusion; D010477:Perfusion; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000889:Anti-Arrhythmia Agents; D000927:Anticonvulsants; D048289:Imidazolidines