Synthesis and biological activity of picobenzide (3,5-dimethyl-N-(pyridin-4-ylmethyl)benzamide) analogues as potential antipsychotic agents

Arzneimittelforschung. 2005;55(12):725-9. doi: 10.1055/s-0031-1296921.

Abstract

A series of analogues related to picobenzide (CAS 51832-87-2) have been prepared and have been used as starting material to obtain new trisubstituted oxazole derivatives. Two compounds showed a promising pharmacological profile in screening tests of antipsychotic activity, since they affected apomorphine-induced hyperactivity without significant effects on stereotypies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antipsychotic Agents / chemical synthesis*
  • Antipsychotic Agents / pharmacology*
  • Apomorphine / antagonists & inhibitors
  • Apomorphine / pharmacology
  • Behavior, Animal / drug effects
  • Benzamides / chemical synthesis*
  • Benzamides / pharmacology*
  • Dopamine Agonists / pharmacology
  • Drug Evaluation, Preclinical
  • Hyperkinesis / chemically induced
  • Hyperkinesis / prevention & control
  • Indicators and Reagents
  • Male
  • Mice
  • Motor Activity / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Stereotyped Behavior / drug effects
  • Structure-Activity Relationship

Substances

  • Antipsychotic Agents
  • Benzamides
  • Dopamine Agonists
  • Indicators and Reagents
  • picobenzide
  • Apomorphine