Yoon, Juhee Yoo, Eun A. Kim, Ji-Yeon Pae, Ae Nim Rhim, Hyewhon Park, Woo-Kyu Kong, Jae Yang Choo, Hea-Young Park 2024-01-20T23:05:43Z 2024-01-20T23:05:43Z 2021-09-03 2008-05-15 0968-0896 https://pubs.kist.re.kr/handle/201004/133490 Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl) propyl] benzene sulfonamides and N-[3-(4- substituted phenyl-piperazine-1-yl) propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT7 receptor antagonists. Most of the compounds showed the IC50 values of 12-580 nM. Four methyl branched analogues were also obtained, but the activity for methyl branched analogues was almost same as its straight chain congeners. Among the synthesized compounds, 3c showed a good activity on 5-HT7 receptors and a good selectivity on 5-HT1a, 5-HT2a, 5-HT2c, and 5-HT6 receptors. (C) 2008 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD POTENT Preparation of piperazine derivatives as 5-HT7 receptor antagonists Article 10.1016/j.bmc.2008.04.023 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.16, no.10, pp.5405 - 5412 BIOORGANIC & MEDICINAL CHEMISTRY 16 10 5405 5412 scie scopus 000256052400005 2-s2.0-43749091957 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article POTENT 5-HT7 receptor antagonists piperazine sulfonamide 5-HT2c receptor antagonists.