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Synthesis, docking studies, and pharmacological evaluation of 2-hydroxypropyl-4-arylpiperazine derivatives as serotoninergic ligands. 2021
Elisa Magli, and
Ewa Kędzierska, and
Agnieszka A Kaczor, and
Anna Bielenica, and
Beatrice Severino, and
Ewa Gibuła-Tarłowska, and
Jolanta H Kotlińska, and
Angela Corvino, and
Rosa Sparaco, and
Giovanna Esposito, and
Stefania Albrizio, and
Elisa Perissutti, and
Francesco Frecentese, and
Anna Leśniak, and
Magdalena Bujalska-Zadrożny, and
Marta Struga, and
Raffaele Capasso, and
Vincenzo Santagada, and
Giuseppe Caliendo, and
Ferdinando Fiorino
Dipartimento di Farmacia, Università degli Studi di Napoli "Federico II", Napoli, Italy.
A new series of norbornene and exo-N-hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide derivatives was prepared, and their affinities to the 5-HT1A , 5-HT2A , and 5-HT2C receptors were evaluated and compared with a previously synthesized series of derivatives characterized by the same nuclei, to identify selective ligands for the subtype receptors. Arylpiperazines represent one of the most important classes of 5-HT1A R ligands, and the research of new derivatives has been focused on the modification of one or more portions of this pharmacophore. The combination of structural elements (heterocyclic nucleus, hydroxyalkyl chain, and 4-substituted piperazine), known to be critical for the affinity to 5-HT1A receptors, and the proper selection of substituents resulted in compounds with high specificity and affinity toward serotoninergic receptors. The most active compounds were selected for further in vivo assays to determine their functional activity. Finally, to rationalize the obtained results, molecular docking studies were performed. The results of the pharmacological studies showed that 3e, 4j, and 4n were the most active and promising derivatives for the serotonin receptor considered in this study.
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