Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands

被引：16

作者：

Frecentese, Francesco ^{[1
]}

Fiorino, Ferdinando ^{[1
]}

Perissutti, Elisa ^{[1
]}

Severino, Beatrice ^{[1
]}

Magli, Elisa ^{[1
]}

Esposito, Antonella ^{[1
]}

De Angelis, Francesca ^{[1
]}

Massarelli, Paola ^{[2
]}

Nencini, Cristina ^{[2
]}

Viti, Barbara ^{[2
]}

Santagada, Vincenzo ^{[1
]}

Caliendo, Giuseppe ^{[1
]}

机构：

[1] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy

[2] Univ Siena, Dipartimento Farmacol G Segre, I-53100 Siena, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 02期

关键词：

Arylpiperazines; Microwave irradiation; Combinatorial chemistry; Serotonin; VITRO PHARMACOLOGICAL EVALUATION; 5-HT1A RECEPTOR LIGANDS; DRUG DISCOVERY; SACCHARINE DERIVATIVES; ASSISTED SYNTHESIS; BINDING; IRRADIATION; BRAIN; BENZOTRIAZINONE; TECHNOLOGY;

D O I：

10.1016/j.ejmech.2009.11.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An easy and convenient microwave-assisted synthesis of a small library of indolic arylpiperazine derivatives is described. Parallel and mixed pool combinatorial methods are reported and compared. The described reactions are nucleophilic substitutions of several aromatic piperazines in presence of K2CO3. Good yields and short reaction times are the main aspect of these procedures. Binding assays shed additional light on the influence of the LCAPs on the 5-HT1A, 5-HT2A and 5-HT2C receptors affinity and allowed to disclose three interesting compounds as 5-HT2C, mixed 5-HT2A/5-HT2C and 5-HT1A/5-HT2C ligands (4i, 4l and 4d, respectively), with potential antiepileptic, anxiolytic or atypical antipsychotic agent therapeutical profiles. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：752 / 759

页数：8