Synthesis and pharmacological properties of new 3-ethoxycarbonyl-11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepines.
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.
Chimirri
A
A
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
Gitto
Rosaria
R
Quartarone
S
S
Orlando
V
V
De Sarro
A
A
De Sarro
G B
GB
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D051379:Mice; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000517:prevention & control; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D018091:Receptors, AMPA; C061950:GYKI 52466; D001569:Benzodiazepines