title: Synthesis, structure and antiarrhythmic properties evaluation of new basic derivatives of 5,5-diphenylhydantoin.
abstract: The synthesis of 1-N and 3-N aminoalkyl derivatives of 5,5-diphenylhydantoin is described. Structural elucidation based on X-ray analysis was performed for two representative compounds 4a and 9b. The effect of tested compounds on the electrocardiogram was examined in vitro in the non-working heart perfusion test and antiarrhythmic activity in the rat coronary artery ligation-reperfusion model. The most active 1-N derivatives 4a and 7b have shown properties of the compounds belonging to class Ia, according to the Vaughan Williams classification. The spatial organisation of the chosen compounds necessary for their pharmacological activity was discussed.
authors.affiliation: Jagiellonian University Medical College, Department of Chemical Technology of Drugs, Medyczna 9, PL 30-688, Kraków, Poland. mfkonono@cyf-kr.edu.pl
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kieć-Kononowicz
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Stadnicka
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Mitka
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Pekala
authors.forename: Barbara
authors.initials: B
authors.lastname: Filipek
authors.forename: Jacek
authors.initials: J
authors.lastname: Sapa
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Zygmunt
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D000927:Anticonvulsants / Q000737:chemistry; D001145:Arrhythmias, Cardiac / Q000188:drug therapy / Q000209:etiology; D018360:Crystallography, X-Ray; D015428:Myocardial Reperfusion Injury / Q000150:complications; D010672:Phenytoin / Q000031:analogs & derivatives* / Q000737:chemistry; D051381:Rats
chemical_list: D000889:Anti-Arrhythmia Agents; D000927:Anticonvulsants; D010672:Phenytoin