Structure-activity relationships of 1,2,4-triazolo[1,5-a] quinoxalines and their 1-deaza analogues imidazo[1,2-a]quinoxalines at the benzodiazepine receptor.
The synthesis, BZR binding activity, and GABA ratio of some 1,2,4-triazolo[1,5-a]quinoxalines and imidazo[1,2-a]quinoxalines are reported. Both series of compounds displayed similar affinities while their efficacies were different. The structure-activity relationships have provided the opportunity to localize on the BZR accessory areas which are able to enhance the affinity and evaluate the importance of the presence or absence of a proton acceptor atom to determine different trends of efficacy.
Catarzi
D
D
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Cecchi
L
L
Colotta
V
V
Melani
F
F
Filacchioni
G
G
Martini
C
C
Giusti
L
L
Lucacchini
A
A
D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002417:Cattle; D005445:Flunitrazepam / Q000378:metabolism; D007093:Imidazoles / Q000138:chemical synthesis / Q000378:metabolism; D066298:In Vitro Techniques; D011810:Quinoxalines / Q000138:chemical synthesis / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000378:metabolism
D007093:Imidazoles; D011810:Quinoxalines; D011963:Receptors, GABA-A; D014230:Triazoles; D005445:Flunitrazepam