1,2,3-triazolo[1,5-a]quinoxalines: synthesis and binding to benzodiazepine and adenosine receptors

被引：51

作者：

Bertelli, L

Biagi, G

Giorgi, I

Manera, C

Livi, O

Scartoni, V

Betti, L

Giannaccini, G

Trincavelli, L

Barili, PL

机构：

[1] Univ Pisa, Dipartimento Sci Farmaceut, I-56126 Pisa, Italy

[2] Univ Pisa, Ist Policattedra Discipline Biol, I-56126 Pisa, Italy

[3] Univ Pisa, Dipartimento Bioorgan, I-56126 Pisa, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 33卷 / 02期

关键词：

1,2,3-triazolo[1,5-a]quinoxalines; benzodiazepine receptor binding; adenosine receptor binding;

D O I：

10.1016/S0223-5234(98)80036-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper reports the synthesis and binding assays toward benzodiazepine and adenosine A(1) and A(2A) receptors of new 1,2,3-triazolo[1,5-a]quinoxalin-4-one derivatives. The prepared compounds show good affinity toward the benzodiazepine receptor (K-i 53-314 nM); the GABA ratio values suggest an inverse agonist activity for the N(5) unsubstituted compounds 6b-d and an agonist activity for the N(5) methylated compounds 7a-c. Some derivatives of both series show good affinity (Ki < 100 nM) and selectivity toward the adenosine A(1) receptorial subtype. (C) Elsevier, Paris.

引用

页码：113 / 122

页数：10