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Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists
- Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists
- Hayat, Faisal; Viswanath, Ambily Nath Indu; Pae, Ae Nim; Rhim, Hyewhon; Park, Woo-Kyu; Choo, Hea-Young Park
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- 0968-0896; 1464-3391
- vol. 23, no. 6, pp. 1313 - 1320
- 4-Nitroindole; Sulfonamides; Methyleneamino-N,N-dimethylformamidine group; 5-HT2A; 5-HT2C; 5-HT6 receptor
- PERGAMON-ELSEVIER SCIENCE LTD
- SCI; SCIE; SCOPUS
- 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.
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