Benzodiazepine receptor ligands.: 4.: Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides

被引：34
|
作者：
Costanzo, A
Guerrini, G
Ciciani, G
Bruni, F
Selleri, S
Costa, B
Martini, C
Lucacchini, A
Aiello, PM
Ipponi, A
机构：
[1] Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
[2] Univ Pisa, Dipartimento Psichiatria Neurolbiol Farmacol & Bi, I-56126 Pisa, Italy
[3] Univ Florence, Dipartimento Farmacol Preclin & Clin Aiazzi Manci, I-50139 Florence, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 42卷 / 12期
关键词：
D O I：
10.1021/jm981126y
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of new 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their binding activities at the central benzodiazepine receptor (BZR) are reported. The derivatives substituted at the 3-position with electron-rich five-membered rings, such as pyrrole 11, 2-thiophene 13c, or 3-thiophene 13d, showed good affinity values for BZR. In in vivo tests the 3-(thien-3-yl)-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide; (13d) showed selective anticonvulsant activity.
引用
收藏
页码：2218 / 2226
页数：9
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