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

Article abstract of DOI:10.1016/j.ejmech.2009.11.023

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-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.