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.

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

GIUSTI, LAURA;LUCACCHINI, ANTONIO;MARTINI, CLAUDIA
1995

Abstract

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.
Ambrogi, V; Grandolini, G; Perioli, L; Giusti, Laura; Lucacchini, Antonio; Martini, Claudia
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/206146
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