Synthesis and pharmacological properties of new 3-ethoxycarbonyl-11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepines

Farmaco. 2002 Sep;57(9):759-63. doi: 10.1016/s0014-827x(02)01272-7.

Abstract

A series of new 3-ethoxycarbonyl-11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepines was synthesized starting from the corresponding bicyclic 1-aryl-3,5-dihydro-7,8-dimethoxy-4H-2,3-benzodiazepin-4-ones (CFMs), previously described as noncompetitive AMPA-type glutamate receptor antagonists, more potent than GYKI 52466. New synthesized compounds proved to be able to protect against seizures induced by means of auditory stimulation in DBA/2 mice and compound 8f the most active of the series showed anticonvulsant properties comparable to GYKI 52466.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / pharmacology
  • Drug Evaluation, Preclinical
  • Mice
  • Receptors, AMPA / antagonists & inhibitors*
  • Seizures / prevention & control
  • Structure-Activity Relationship

Substances

  • Anti-Anxiety Agents
  • Anticonvulsants
  • Receptors, AMPA
  • GYKI 52466
  • Benzodiazepines