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

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.

• Authors: A Chimirri, Rosaria Gitto, S Quartarone, V Orlando, A De Sarro, G B De Sarro
• Journal: Farmaco (Societa chimica italiana : 1989) (Farmaco) Vol. 57 Issue 9 Pg. 759-63 (Sep 2002) ISSN: 0014-827X [Print] France
• PMID: 12385527 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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