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KMID : 0617320080190010032
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Journal of Pharmacetical Sceiences Ewha Womans University
2008 Volume.19 No. 1 p.32 ~ p.39
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Preparation of piperazine derivatives as 5-HT_(7) receptor antagonists
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Yoon Ju-Hee
Park Choo Hea-Young
Rhim Hye-Won
Park Woo-Kyu
Kong Jae-Yang
Pae Ae-Nim
Yoo Eun-A
Kim Ji-Yeon
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Abstract
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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 12-580 nM. 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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KEYWORD
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5-HT_(7) receptor antagonists, Piperazine, Sulfonamid, 5-HT_(2c) receptor antagonists
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