New 4-arylaminopiperidines with antihypoxic and anticonvulsive activity

Arzneimittelforschung. 1994 Sep;44(9):989-91.

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.

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology
  • Cell Survival / drug effects
  • Cyanides / pharmacology
  • Hypoxia / chemically induced
  • Hypoxia / drug therapy*
  • Male
  • Mice
  • Mice, Inbred Strains
  • Pentylenetetrazole
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology
  • Seizures / chemically induced
  • Seizures / prevention & control
  • Thiazoles / pharmacology

Substances

  • Anticonvulsants
  • Cyanides
  • Piperidines
  • Thiazoles
  • sabeluzole
  • Pentylenetetrazole