Up to date a number of compounds have been found to bind to 5-HT₇ receptors. One of the class of ligands are arylsulfonamides connected by the three or four methylene groups spacer with 4-substituted tetrahydropirydine, 1-arylpiperazine or tetrahydroisoquinoline fragments. Because these structural features are common with other G-coupled receptors ligands, mainly 5-HT_1A ones, searching for the new 5-HT₇ ligands raises the problem of selectivity.

As a part of our ongoing project to identify new compounds with potential antidepressant activity, we designed series of azinesulfonamides containing different tertiary amines.

Herein, we disclose their synthesis and preliminary biological evaluation as 5-HT_1A and 5-HT₇ receptor ligands. Starting azinesulfonylchlorides were synthesized according to the previously reported method.³

 This study was partly supported by the Polish Ministry of Science and Higher Education (MNiSW), Grant No. N N405 378437

 References:

1. Pittala, V.; Salerno, L.; Modica, M.; Siracusa, M.A.; Romeo, G. Mini Rev Med Chem 2007, 7, 945-960.

2. Mnie-Filali, O.; Lambas-Senas, L.; Zimmer, L.; Haddjeri, N. Drug News Perspect 2007, 20, 613-618.

3. Marciniec, K.; Maślankiewicz, A.; Pawłowski, M.; Zajdel, P. Heterocycles, 2007, 71, 1975-1990.

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