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  • Title: Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.
    Author: Hayat F, Viswanath AN, Pae AN, Rhim H, Park WK, Choo HY.
    Journal: Bioorg Med Chem; 2015 Mar 15; 23(6):1313-20. PubMed ID: 25684421.
    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 1μM, 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.
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