| 18456500 |
Yoon J, Yoo EA, Kim JY, Pae AN, Rhim H, Park WK, Kong JY, Park Choo HY: Preparation of piperazine derivatives as 5-HT7 receptor antagonists. . Bioorg Med Chem. 2008 May 15;16(10):5405-12. Epub 2008 Apr 15.
Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl) propyl] benzene sulfonamides and N-[3-(4-substituted phenyl-piperazine-1-yl) propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT (7) receptor antagonists. Most of the compounds showed the IC (50) values of 12-580nM. Four methyl branched analogues were also obtained, but the activity for methyl branched analogues was almost same as its straight chain congeners. Among the synthesized compounds, 3c showed a good activity on 5-HT (7) receptors and a good selectivity on 5-HT (1a), 5-HT (2a), 5-HT (2c), and 5-HT (6) receptors. |
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