Synthesis and anticonvulsant properties of tetrahydroisoquinoline derivatives.
As a follow up of our previous structure-activity relationship and molecular modeling studies, we synthesized a novel series of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as potential non-competitive AMPA receptor antagonists. When tested for their ability to prevent sound-induced seizures in DBA/2 mice, some of these novel compounds showed high anticonvulsant potency.
Gitto
Rosaria
R
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168, Messina, Italy. rgitto@pharma.unime.it
Caruso
Roberta
R
Orlando
Valerie
V
Quartarone
Silvana
S
Barreca
Maria Letizia
ML
Ferreri
Guido
G
Russo
Emilio
E
De Sarro
Giovambattista
G
Chimirri
Alba
A
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines / Q000494:pharmacology; D001570:Benzodiazepinones / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology; D005260:Female; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D008958:Models, Molecular; D015394:Molecular Structure; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors; D012640:Seizures / Q000517:prevention & control*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000927:Anticonvulsants; D001570:Benzodiazepinones; C119033:CFM 2; D018691:Excitatory Amino Acid Antagonists; D018091:Receptors, AMPA; D044005:Tetrahydroisoquinolines; C061950:GYKI 52466; D001569:Benzodiazepines; C085266:talampanel