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Synthesis and pharmacological properties of new 3-ethoxycarbonyl-11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepines
Authors:Chimirri A  Gitto Rosaria  Quartarone S  Orlando V  De Sarro A  De Sarro G B
Affiliation:Dipartimento Farmaco-Chimico, Università di Messina, Italy.
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.
Keywords:AMPA receptor antagonists   3-Ethoxycarbonyl-11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepines   Anticonvulsant agents
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