A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABAA) receptor subtype ligand: synthesis and pharmacological evaluation

被引：9

作者：

Guerrini, Gabriella ^{[1
]}

Ciciani, Giovanna ^{[1
]}

Daniele, Simona ^{[2
]}

Martini, Claudia ^{[2
]}

Costagli, Camilla ^{[1
]}

Guarino, Chiara ^{[1
]}

Selleri, Silvia ^{[1
]}

机构：

[1] Univ Firenze, Sez Farmaceut & Nutraceut, Dipartimento NEUROFARBA, Via Ugo Schiff 6, Florence, Italy

[2] Univ Pisa, Dipartimento Farm, Pisa, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2018年 / 26卷 / 09期

关键词：

BENZODIAZEPINE-RECEPTOR; BIOLOGICAL EVALUATION; BZR AFFINITY; DERIVATIVES;

D O I：

10.1016/j.bmc.2018.04.011

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A comparison between compounds with pyrazolo[1,5-a]pyrimidine structure (series 4-6) and pyrazolo [5,1-c][1,2,4]triazine core (series 9) as ligands at GABA(A)-receptor subtype, was evaluated. Moreover, for pyrazolotriazine derivatives having binding recognition, the interaction on recombinant rat alpha(1-3,5) GABA(A) receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as alpha 1-selective and 9h as alpha 2-selective ligands. (C) 2018 Elsevier Ltd. All rights reserved.

引用

页码：2475 / 2487

页数：13

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