Hayat, Faisal Viswanath, Ambily Nath Indu Pae, Ae Nim Rhim, Hyewhon Park, Woo-Kyu Choo, Hea-Young Park 2024-01-20T07:32:13Z 2024-01-20T07:32:13Z 2021-09-05 2015-03-15 0968-0896 https://pubs.kist.re.kr/handle/201004/125662 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. English PERGAMON-ELSEVIER SCIENCE LTD CYS23SER POLYMORPHISM SEROTONIN LIGANDS BINDING RAT Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists Article 10.1016/j.bmc.2015.01.032 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.6, pp.1313 - 1320 BIOORGANIC & MEDICINAL CHEMISTRY 23 6 1313 1320 scie scopus 000349967600010 2-s2.0-84923534690 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article CYS23SER POLYMORPHISM SEROTONIN LIGANDS BINDING RAT 4-Nitroindole Sulfonamides Methyleneamino-N,N-dimethylformamidine group 5-HT2A 5-HT2C 5-HT6 receptor