Tricyclic heteroaromatic systems. Pyrazolo[3,4-c]quinolin-4-ones and pyrazolo[3,4-c]quinoline-1,4-diones: Synthesis and benzodiazepine receptor activity

被引：13
|
作者：
Catarzi, D
Colotta, V
Varano, F
Cecchi, L
Filacchioni, G
Galli, A
Costagli, C
机构：
[1] Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
[2] Univ Florence, Dipartimento Farmacol Preclin & Clin, I-50134 Florence, Italy
来源：
ARCHIV DER PHARMAZIE | 1997年 / 330卷 / 12期
关键词：
pyrazolo[3,4-c]quinolines, synthesis; benzodiazepine receptor activity;
D O I：
10.1002/ardp.19973301205
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Some pyrazolo[3,4-c]quinoline-4-ones 1-14 and pyrazolo[3,4-c]-quinoline-1,4-diones 15-17 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The moderate binding activity of 1-5, 7, 9-10, 13 is attributable to the lack of the optional proton acceptor at position-1, while the inactivity of the 1,4-dione derivatives 15-17 is due to the lack of the essential proton acceptor at position-3. These conclusions confirm the validity of our proposed pharmacophoric model.
引用
收藏
页码：383 / 386
页数：4
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