Synthesis and preliminary pharmacological evaluation of thiophene analogues of viloxazine as potential antidepressant drugs

Bioorg Med Chem. 1999 Jul;7(7):1349-59. doi: 10.1016/s0968-0896(99)00070-x.

Abstract

A series of eight thienyloxymethylmorpholines, thiophene analogues of viloxazine, have been synthesized by three different routes. The preliminary pharmacological evaluation of this series shows antidepressant properties on the mice models used with a light sedative action. The structure-activity relationship is established in a first approximation.

Publication types

  • Comparative Study

MeSH terms

  • 5-Hydroxytryptophan / pharmacology
  • Animals
  • Antidepressive Agents / chemical synthesis*
  • Antidepressive Agents / pharmacology*
  • Apomorphine / toxicity
  • Blepharoptosis / chemically induced
  • Blepharoptosis / drug therapy
  • Dose-Response Relationship, Drug
  • Female
  • Hypothermia / chemically induced
  • Hypothermia / drug therapy
  • Imipramine / pharmacology
  • Lethal Dose 50
  • Male
  • Mice
  • Movement Disorders / drug therapy
  • Pentobarbital / pharmacology
  • Sleep / drug effects
  • Structure-Activity Relationship
  • Tetrabenazine / toxicity
  • Viloxazine / analogs & derivatives*

Substances

  • Antidepressive Agents
  • Viloxazine
  • 5-Hydroxytryptophan
  • Pentobarbital
  • Apomorphine
  • Imipramine
  • Tetrabenazine