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Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands. 2010
Francesco Frecentese, and
Ferdinando Fiorino, and
Elisa Perissutti, and
Beatrice Severino, and
Elisa Magli, and
Antonella Esposito, and
Francesca De Angelis, and
Paola Massarelli, and
Cristina Nencini, and
Barbara Viti, and
Vincenzo Santagada, and
Giuseppe Caliendo
Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli, Via D Montesano 49, 80131 Naples, Italy.
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 K(2)CO(3). 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-HT(1A), 5-HT(2A) and 5-HT(2C) receptors affinity and allowed to disclose three interesting compounds as 5-HT(2C), mixed 5-HT(2A)/5-HT(2C) and 5-HT(1A)/5-HT(2C) ligands (4i, 4l and 4d, respectively), with potential antiepileptic, anxiolytic or atypical antipsychotic agent therapeutical profiles.
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