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

R Perrone, F Berardi, NA Colabufo, V Tortorella…

Index: Perrone; Berardi; Colabufo; Tortorella; Fornaretto; Caccia; McArthur European Journal of Medicinal Chemistry, 1997 , vol. 32, # 9 p. 739 - 746

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Citation Number: 7

Abstract

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.