Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7 (4H)-one derivatives as potential GABAA-R ligands

被引：19

作者：

Guerrini, Gabriella ^{[1
]}

Ciciani, Giovanna ^{[1
]}

Daniele, Simona ^{[2
]}

Mannelli, Lorenzo Di Cesare

Ghelardini, Carla

Martini, Claudia ^{[2
]}

Selleri, Silvia ^{[1
]}

机构：

[1] Univ Firenze, Dipartimento NEUROFARBA, Sez Farmaceut & Nutraceut, Via Ugo Schiff 6, I-50019 Florence, Italy

[2] Univ Pisa, Dipartimento Farm, Via Bonanno 6, I-56126 Pisa, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2017年 / 25卷 / 06期

关键词：

Drug design; GABA(A); Pyrazolo[1,5-a]pyrimidin-7(4H)one; Receptor; BENZODIAZEPINE-RECEPTOR LIGANDS; BZR AFFINITY; 5-OXIDE; SUBTYPE; SYSTEM; INHIBITOR; RODENTS; BINDING;

D O I：

10.1016/j.bmc.2017.02.013

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：

The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABA(A)-receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30 mg/kg. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：1901 / 1906

页数：6

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