Synthesis of disubstituted 1,4-diazepines with affinity to GABAA-receptor subtypes

被引：9

作者：

Briel, D. ^{[1
]}

Rudolph, I.

Unverferth, K. ^{[2
]}

Mann, S.

机构：

[1] Univ Leipzig, Inst Pharm, Bereich Pharmazeut Chem, D-04103 Leipzig, Germany

[2] Biotie Therapies GmbH, Radebeul, Germany

来源：

PHARMAZIE | 2010年 / 65卷 / 09期

关键词：

BENZODIAZEPINE SITE LIGANDS; GABA(A) RECEPTOR SUBTYPES; DEHYDROACETIC ACID; CRYSTAL-STRUCTURES; DERIVATIVES; CONDENSATION; MODULATORS; COPPER(II); NICKEL(II); EFFICACY;

D O I：

10.1691/ph.2010.0559

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of tetrahydro-1H-1,4-diazepines 4a-c, dihydro-1H-1,4-diazepine 5 and pyrido diazepines 8 and 10 was prepared. Originated form dehydroacetic acid (DHA) and aromatic aldehydes cinnamoyl compounds 3a-c were obtained and converted with ethylenediamine to give tetrahydro-1H-1,4-diazepines 4a-c. For the synthesis of pyrido[1,2-d][1,4]diazepines 8 and 10 a new snythetic approach is described. Compounds 4b and 5 were investigated concerning their affinity to different benzodiazepine receptor subtypes. The determined IC50 values for 5 are 1.5 mu M and 1.1 mu M at 10 mu M respectively.

引用

页码：641 / 644

页数：4

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