Hayat, Faisal Cho, Sungjin Rhim, Hyewhon Viswanath, Ambily Nath Indu Pae, Ae Nim Lee, Jae Yeol Choo, Dong Joon Choo, Hea-Young Park 2024-01-20T11:32:56Z 2024-01-20T11:32:56Z 2021-09-04 2013-09-01 0968-0896 https://pubs.kist.re.kr/handle/201004/127679 The exclusive distribution of 5-HT6 receptor in the brain regions and high affinity for antipsychotic and antidepressant drugs makes 5-HT6 receptor a promising target in treatment of CNS diseases. Based on a pharmacophore model reported in the literature, we designed and synthesized a novel series of 5-HT6 receptor ligands having indole as a central aromatic core and 1-amino-4-methyl piperazine as positive ionizable group. Out of 32 compounds we have successfully identified 10 new compounds as 5-HT6 receptor antagonists. The structure-activity relationship (SAR) studies have been carried out by mapping the compounds with the 3D QSAR model. (C) 2013 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD MEMORY FORMATION ANTAGONISTS POTENT Design and synthesis of novel series of 5-HT6 receptor ligands having indole, a central aromatic core and 1-amino-4 methyl piperazine as a positive ionizable group Article 10.1016/j.bmc.2013.05.051 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.21, no.17, pp.5573 - 5582 BIOORGANIC & MEDICINAL CHEMISTRY 21 17 5573 5582 scie scopus 000323294600075 2-s2.0-84881376737 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article MEMORY FORMATION ANTAGONISTS POTENT 5-HT6 receptor antagonist 1-Amino-4-methylpiperazine Sulfonyl indole 3D QSAR Pharmacophore mapping