title: New 4-arylaminopiperidines with antihypoxic and anticonvulsive activity.
abstract: Several new bioanalogues of (+/-)-N-methyl-N-(1-[3-(4-fluorophenoxy)-2-hydroxy-propyl]piperidin++ +-4-yl) benzothiazol-2-amine (1, sabeluzole, CAS 104383-17-7) were prepared by reacting 1,2-epoxy-3-aryloxypropanes with 4-arylaminopiperidines. Some of these derivatives showed enhanced activity in the potassium cyanide hypoxia test and in the pentetrazol convulsion test in mice compared to 1.
authors.affiliation: Chemical Works of Gedeon Richter Ltd., Budapest, Hungary.
authors.forename: G
authors.initials: G
authors.lastname: Domány
authors.forename: G
authors.initials: G
authors.lastname: Barta-Szalai
authors.forename: E
authors.initials: E
authors.lastname: Pálosi
authors.forename: S
authors.initials: S
authors.lastname: Szabó
authors.forename: I
authors.initials: I
authors.lastname: Schön
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D003486:Cyanides / Q000494:pharmacology; D000860:Hypoxia / Q000139:chemically induced / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010433:Pentylenetetrazole; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013844:Thiazoles / Q000494:pharmacology
chemical_list: D000927:Anticonvulsants; D003486:Cyanides; D010880:Piperidines; D013844:Thiazoles; C055163:sabeluzole; D010433:Pentylenetetrazole