New 4-arylaminopiperidines with antihypoxic and anticonvulsive activity.
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.
Domány
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G
Chemical Works of Gedeon Richter Ltd., Budapest, Hungary.
Barta-Szalai
G
G
Pálosi
E
E
Szabó
S
S
Schön
I
I
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
D000927:Anticonvulsants; D003486:Cyanides; D010880:Piperidines; D013844:Thiazoles; C055163:sabeluzole; D010433:Pentylenetetrazole