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Preparation of piperazine derivatives as 5-HT7 receptor antagonists

Title
Preparation of piperazine derivatives as 5-HT7 receptor antagonists
Authors
Yoon J.Yoo E.A.Kim J.-Y.Pae A.N.Rhim H.Park W.-K.Kong J.Y.Park Choo H.-Y.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 16, no. 10, pp. 5405 - 5412
Indexed
SCI; SCIE; SCOPUS WOS scopus
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-HT7 receptor antagonists. Most of the compounds showed the IC50 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-HT7 receptors and a good selectivity on 5-HT1a, 5-HT2a, 5-HT2c, and 5-HT6 receptors. © 2008 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2008.04.023
Appears in Collections:
약학대학 > 약학과 > Journal papers
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