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 interni: | |
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 |
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