Tricyclic heteroaromatic systems 1,2,4-triazolo[1,5-a]quinoxalines: synthesis and benzodiazepine receptor activity.
The synthesis, the benzodiazepine binding activity and the "in vitro" biological effect of some 1,2,4-triazolo[1,5-a]quinoxalines, 3-aza-analogues of some previously reported pyrazolo[1,5-a]quinoxalines, are described. Molecular modelling is used to define the structural requirements of the benzodiazepine recognition site which influence the affinity and different efficacy of these rigid ligands.
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; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002707:Chlordiazepoxide / Q000494:pharmacology; D005445:Flunitrazepam / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D011810:Quinoxalines; D011963:Receptors, GABA-A; D014230:Triazoles; D005445:Flunitrazepam; D002707:Chlordiazepoxide