The synthesis of three series of 1- and 2-substituted imidazo[2,1-d][1,5]benzothiazepines is accomplished starting from 1,5-benzothiazepin-4-ones. All the synthesized compounds were evaluated for their affinity for the benzodiazepine receptor, testing their ability to displace [H-3]Flunitrazepam from bovine brain membrane protein. A few of the tested compounds showed good affinity, in particular compound 9a (K-i = 43.00 nM). The GABA-ratio of the active compounds suggests an antagonist or partial agonist activity. The data obtained allow us to draw some comments on the structure-activity relationships.
|Autori:||AMBROGI V; GRANDOLINI G; PERIOLI L; GIUSTI L; LUCACCHINI A; MARTINI C|
|Titolo:||STUDIES ON ANNULATED 1,4-BENZOTHIAZINES AND 1,5-BENZOTHIAZEPINES .9. IMIDAZO[2,1-D][1,5]BENZOTHIAZEPINES - SYNTHESIS AND IN-VITRO BENZODIAZEPINE RECEPTOR AFFINITY|
|Anno del prodotto:||1995|
|Digital Object Identifier (DOI):||10.1016/0223-5234(96)88253-5|
|Appare nelle tipologie:||1.1 Articolo in rivista|