Synthesis and anticonvulsant activity of N-3 substituted 2,3-benzodiazepines.
A series of new 3-alkylcarbamoyl-1-aryl-3,5-dihydro-7,8-dimethoxy-4H-2,3-benzodiazepin-4-ones was synthesized starting from the corresponding 3-N-unsubstituted derivatives, previously described as noncompetitive AMPA-type glutamate receptor antagonists. The new compounds proved to protect against seizures induced by means of auditory stimulation in DBA/2 mice and some of them showed anticonvulsant properties comparable or better than those of GYKI 52466, the prototype of 2,3-benzodiazepine noncompetitive AMPA receptor antagonists.
Quartarone
Silvana
S
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. silvanaquartarone@libero.it
Caruso
Roberta
R
Orlando
Valèrie
V
Russo
Emilio
E
De Sarro
Giovambattista
G
Chimirri
Alba
A
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051379:Mice; D008811:Mice, Inbred DBA; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000188:drug therapy* / Q000517:prevention & control; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D018091:Receptors, AMPA; C061950:GYKI 52466; D001569:Benzodiazepines