Synthesis of arylpiperazines with a terminal naphthothiazole group and their evaluation on 5-HT, DA and a receptor

Abstract

Summary The synthesis, affinities for 5-HT1A, 5-HT2, D, D2, α1 and α2 receptors and structure-activity relationships are described for a series of arylpiperazines substituted on the N-4 atom with an ω-(2-naphthothiazole)alkyl chain. The best affinity for 5-HT1A receptors was obtained for 1-(2-methoxyphenyl)piperazine derivatives with IC50 values in the range 3.2–12 nM; however, for all the reported compounds mixed 5-HT1A/D2/α affinities were observed.