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
- 배애님; 임혜원; Faisal Hayat; Ambily Nath Indu Viswanath; 박우규; 박혜영
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 23, NO 6-1320
- 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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