STRUCTURE-ACTIVITY-RELATIONSHIPS OF 1,2,4-TRIAZOLO[1,5-A]QUINOXALINES AND THEIR 1-DEAZA ANALOGS IMIDAZO[1,2-A]QUINOXALINES AT THE BENZODIAZEPINE RECEPTOR

被引：37

作者：

CATARZI, D

CECCHI, L

COLOTTA, V

MELANI, F

FILACCHIONI, G

MARTINI, C

GIUSTI, L

LUCACCHINI, A

机构：

[1] UNIV FLORENCE,DIPARTIMENTO SCI FARMACEUT,I-50121 FLORENCE,ITALY

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 18期

关键词：

D O I：

10.1021/jm00044a004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis, BZR binding activity, and GABA ratio of some 1,2,4-triazolo[1,5-a]quinoxalines and imidazo[l,2-a]quinoxalines are reported. Both series of compounds displayed similar affinities while their efficacies were different. The structure-activity relationships have provided the opportunity to localize on the BZR accessory areas which are able to enhance the affinity and evaluate the importance of the presence or absence of a proton acceptor atom to determine different trends of efficacy.

引用

页码：2846 / 2850

页数：5

共 29 条

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