title: Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.
abstract: 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.
authors: Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli, Via D Montesano 49, 80131 Naples, Italy.
authors: Francesco
authors: F
authors: Frecentese
authors: Ferdinando
authors: F
authors: Fiorino
authors: Elisa
authors: E
authors: Perissutti
authors: Beatrice
authors: B
authors: Severino
authors: Elisa
authors: E
authors: Magli
authors: Antonella
authors: A
authors: Esposito
authors: Francesca
authors: F
authors: De Angelis
authors: Paola
authors: P
authors: Massarelli
authors: Cristina
authors: C
authors: Nencini
authors: Barbara
authors: B
authors: Viti
authors: Vincenzo
authors: V
authors: Santagada
authors: Giuseppe
authors: G
authors: Caliendo
mesh_terms: D000818:Animals; D020650:Combinatorial Chemistry Techniques; D004353:Drug Evaluation, Preclinical; D007211:Indoles / Q000737:chemistry*; D008024:Ligands; D008297:Male; D008872:Microwaves; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011985:Receptors, Serotonin / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism*
chemical_list: D007211:Indoles; D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; D000077489:Piperazine; D012701:Serotonin; C030374:indole