Benzodiazepine receptor ligands -: III.: Synthesis and biological evaluation of 2-and/or 3-substituted pyrazolo[5,1-c][l,2,4]benzotriazine 5-oxides

被引：13
|
作者：
Guerrini, G
Costanzo, A
Bruni, F
Ciciani, G
Selleri, S
Gratteri, P
Costa, B
Martini, C
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：
FARMACO | 1999年 / 54卷 / 06期
关键词：
2 and/or 3-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide; benzodiazepine receptor; receptor binding;
D O I：
10.1016/S0014-827X(99)00044-0
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A new series of 2- and/or 3-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their 8-chloro derivatives were synthesized, and their benzodiazepine receptor (BZR) affinities were evaluated in vitro in comparison to lead compound 3-ethoxycarbonyl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine-5-oxide (29) [1,2]. None of the new compounds showed significant affinity for BZR. On the basis of a pharmacophore/receptor model suggested for lead compound 29, some hypotheses to explain the inactivity of new derivatives are discussed. (C) 1999 Elsevier Science S.A. All rights reserved.
引用
收藏
页码：375 / 389
页数：15
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