The class of arylpiperazines have been largely investigated as a group of compounds according to their ability to modify serotonergic neurotransmission via 5HT_1A receptor interactions.

Searching for new chemical substances expected to have an anxiety-relieving character, we have designed a new series of 4-[4-aryl/heteroarylpiperazin-1-ylbutyl) derivatives of 3-phenylpiperidine-2,6-dione 2, analoges of gepirone [1,2].

By alkylation of compound 2 with 1,4-dibromobutane, 4-(4-bromobutyl) substituted derivative 3 was obtained. Next the latter was condensed with appropriate amines to yield compounds 6-10.

The structure of all derivatives of compound 2 have been established on the basis of elemental analysis and ¹H NMR spectra.

Compounds 4 and 6 were given to the Department of Crystalography, UMCS in Lublin, for X-ray single-crystal analysis, performed by prof. dr hab. A.E. Kozioł.

Several compounds were given to the Department of Toxicology, The Medical University of Lublin, for pharmacological screenings, performed by prof. dr hab. E. Jagiełło-Wójtowicz.

References

1. M. H. Paluchowska et al., Novel, flexible and conformationally defined analogs of gepirone: synthesis and 5-HT_1A, 5-HT_2A and D₂ receptor activity; Bioorg. Med. Chem., 2005, 13(4),1195-200.
2. M.L.Lopez-Rodriguez et al., Arylpiperazine derivatives acting at 5-HT_1A receptors; Current Medicinal Chemistry, 2002, 9, 443-469.

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