Yoo, Euna Yoon, Juhee Pae, Ae Nim Rhim, Hyewhon Park, Woo-Kyu Kong, Jae Yang Choo, Hea-Young Park 2024-01-20T20:00:39Z 2024-01-20T20:00:39Z 2021-09-02 2010-02-15 0968-0896 https://pubs.kist.re.kr/handle/201004/131713 A novel series of 5-HT2A ligands that contain a (phenylpiperazinyl-propyl)arylsulfonamides skeleton was synthesized. Thirty-seven N-(cycloalkylmethyl)-4-methoxy-N-(3-(4-arylpiperazin-1-yl)propyl)arylsulfonamide and N-(4-(4-arylpiperazin-1-yl)butan-2-yl)-arylsulfonamide compounds were obtained. The binding of these compounds to the 5-HT2A, 5-HT2C, and 5-HT7 receptors was evaluated. Most of the compounds showed IC50 values of less than 100 nM and exhibited high selectivity for the 5-HT2A receptor. Among the synthesized compounds, 16a and 16d showed good affinity at 5-HT2A (IC50 = 0.7 nM and 0.5 nM) and good selectivity over 5-HT2C (50-100 times) and 5-HT7 (1500-3000 times). (C) 2010 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD SEROTONIN DERIVATIVES SCHIZOPHRENIA AFFINITY Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT2A receptor antagonists Article 10.1016/j.bmc.2009.12.067 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.18, no.4, pp.1665 - 1675 BIOORGANIC & MEDICINAL CHEMISTRY 18 4 1665 1675 scie scopus 000274425500032 2-s2.0-75849120790 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article SEROTONIN DERIVATIVES SCHIZOPHRENIA AFFINITY 5-HT2A receptor antagonists Piperazine Sulfonamide