Synthesis, conformational analysis and antidepressant activity of moclobemide new analogues

Pharm Acta Helv. 1997 Apr;72(2):119-22. doi: 10.1016/s0031-6865(97)00004-6.

Abstract

Three new analogues of moclobemide are synthesized. Antidepressant activity of compounds assayed by the Porsolt method reveals that the morpholine ring in moclobemide is one of the key structural parts necessary for antidepressant activity. Superimposition of norepinephrine and gauche forms of serotonin and mociobemide suggest that the phenyl ring, electronegative group attached to the aromatic ring and the amine terminal group may serve as the recognition elements for binding to monoamine oxidase-A (MAO-A).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antidepressive Agents / chemical synthesis*
  • Antidepressive Agents / metabolism
  • Antidepressive Agents / pharmacology*
  • Benzamides / chemical synthesis*
  • Benzamides / metabolism
  • Benzamides / pharmacology*
  • Moclobemide
  • Molecular Conformation
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / chemical synthesis*
  • Monoamine Oxidase Inhibitors / metabolism
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antidepressive Agents
  • Benzamides
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase
  • Moclobemide