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Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists

Title
Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists
Authors
Yoo E.Yoon J.Pae A.N.Rhim H.Park W.-K.Kong J.Y.Park Choo H.-Y.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 18, no. 4, pp. 1665 - 1675
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A novel series of 5-HT2A ligands that contain a (phenylpiperazinyl-propyl)arylsulfonamides skeleton was synthesized. Thirty-seven N-(cycloalkylmethyl)-4-methoxy-N-(3-(4-arylpiperazin-1-yl)propyl)-arylsulfonamide and N-(4-(4-arylpiperazin-1-yl)butan-2-yl)-arylsulfonamide compounds were obtained. The binding of these compounds to the 5-HT2A, 5-HT2C, and 5-HT7 receptors was evaluated. Most of the compounds showed IC50 values of less than 100 nM and exhibited high selectivity for the 5-HT2A receptor. Among the synthesized compounds, 16a and 16d showed good affinity at 5-HT2A (IC50 = 0.7 nM and 0.5 nM) and good selectivity over 5-HT2C (50-100 times) and 5-HT7 (1500-3000 times). © 2010 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2009.12.067
Appears in Collections:
약학대학 > 약학과 > Journal papers
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