Tehran University of Medical Sciences
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Abbas Shafiee

Design and synthesis of 4H-3-(2-phenoxy)phenyl-1,2,4-triazole derivatives as benzodiazepine receptor agonists.


Authors: Akbarzadeh T , Tabatabai SA , Khoshnoud MJ , Shafaghi B , Shafiee A ,
Bioorganic & medicinal chemistry , Vol., No. 0968-0896 (Print) , 20030122 ,Page:0
A series of new 5-substituted analogues of 4H-3-(2-phenoxy)phenyl-1,2,4-triazole and its chlorinated derivatives was designed and prepared. Conformational analysis and superimposition of energy minima conformers of the compounds on estazolam, a known benzodiazepine receptor agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. Rotarod and pentylenetetrazole-induced lethal convulsion tests showed that the introduction of an amino group in position 5 of 1,2,4-triazole ring especially in chlorinated derivatives had the best effect which was comparable with diazepam.