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Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists

Title
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists
Authors
Hayat, FaisalViswanath, Ambily Nath InduPae, Ae NimRhim, HyewhonPark, Woo-KyuChoo, Hea-Young Park
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2015
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link1464-3391JCR Link
Citation
vol. 23, no. 6, pp. 1313 - 1320
Keywords
4-NitroindoleSulfonamidesMethyleneamino-N,N-dimethylformamidine group5-HT2A5-HT2C5-HT6 receptor
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A novel series of 4-nitroindole sulfonamides containing a methyleneamino-N,N-dimethylformamidine were prepared. The binding of these compounds to 5-HT2A and 5-HT2C was evaluated, and most of the compounds showed IC50 values of less than 1 mu M, and exhibited high selectivity for the 5-HT2C receptor. However, little selectivity was observed in the functional assay for 5-HT6 receptors. The computational modeling studies further validated the biological results and also demonstrated a reasonable correlation between the activity of compounds and the mode of superimposition with specified pharmacophoric features. (C) 2015 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2015.01.032
Appears in Collections:
약학대학 > 약학과 > Journal papers
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