Synthesis and pharmacological evaluation of pyrazolo1,5-apyrimidin-7 (4H)-one derivatives as potential GABA(A)-R ligands

Guerrini Gabriella; Ciciani Giovanna; Daniele SimonaMannelli Lorenzo Di CesareGhelardini CarlaMartini ClaudiaSelleri Silvia

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Synthesis and pharmacological evaluation of pyrazolo1,5-apyrimidin-7 (4H)-one derivatives as potential GABA(A)-R ligands

机译：Synthesis and pharmacological evaluation of pyrazolo1,5-apyrimidin-7 (4H)-one derivatives as potential GABA(A)-R ligands

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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.

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《Bioorganic and medicinal chemistry》 |2017年第6期|1901-1906|共6页
作者
Guerrini Gabriella; Ciciani Giovanna; Daniele SimonaMannelli Lorenzo Di CesareGhelardini CarlaMartini ClaudiaSelleri Silvia;
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作者单位

Univ Pisa, Dipartimento Farm, Via Bonanno 6, I-56126 Pisa, Italy;

Univ Firenze, Dipartimento NEUROFARBA, Sez Farmaceut & Nutraceut, Via Ugo Schiff 6, I-50019;

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正文语种英语
中图分类药学;
关键词
Drug design; GABA(A); Pyrazolo1; 5-apyrimidin-7(4H)one; Receptor;

Synthesis and pharmacological evaluation of pyrazolo1,5-apyrimidin-7 (4H)-one derivatives as potential GABA(A)-R ligands

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