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.
Keywords: 4-Nitroindole; 5-HT(2A); 5-HT(2C); 5-HT(6) receptor; Methyleneamino-N,N-dimethylformamidine group; Sulfonamides.
Copyright © 2015 Elsevier Ltd. All rights reserved.