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

被引：20

作者：

AMBROGI, V ^{[1
]}

GRANDOLINI, G ^{[1
]}

PERIOLI, L ^{[1
]}

GIUSTI, L ^{[1
]}

LUCACCHINI, A ^{[1
]}

MARTINI, C ^{[1
]}

机构：

[1] UNIV PISA,IST POLICATTEDRA DISCIPLINE BIOL,I-56100 PISA,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 05期

关键词：

IMIDAZO[2,1-D][1,5]BENZOTHIAZEPINE; BENZODIAZEPINE RECEPTOR AFFINITY; STRUCTURE-ACTIVITY RELATIONSHIP;

D O I：

10.1016/0223-5234(96)88253-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：429 / 437

页数：9

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