103965-93-1Relevant articles and documents
Studies on annulated 1,4-benzothiazines and 1,5-benzothiazepines. IX. Imidazobenzothiazepines: synthesis and in vitro benzodiazepine receptor affinity
Ambrogi, V.,Grandolini, G.,Perioli, L.,Giusti, L.,Lucacchini, A.,Martini, C.
, p. 429 - 439 (1995)
The synthesis of three series of 1- and 2-substituted imidazobenzothiazepines 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 Flunitrazepam from bovine brain membrane protein.A few of the tested compounds showed good affinity, in particular compound 9a (Ki = 43.00 nM).The GABA-ratio of the active compounds suggest an antagonist or partial agonist activity.The data obtained allow us to draw some comments on the structure-activity relationships. imidazobenzothiazepine / benzodiazepine receptor affinity / structure-activity relationship