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Preparation of piperazine derivatives as 5-HT7 receptor antagonists.

作者信息

Yoon Juhee, Yoo Eun A, Kim Ji-Yeon, Pae Ae Nim, Rhim Hyewhon, Park Woo-Kyu, Kong Jae Yang, Park Choo Hea-Young

机构信息

School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.

出版信息

Bioorg Med Chem. 2008 May 15;16(10):5405-12. doi: 10.1016/j.bmc.2008.04.023. Epub 2008 Apr 15.

DOI:10.1016/j.bmc.2008.04.023
PMID:18456500
Abstract

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.

摘要

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