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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 |
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| Authors: | Faisal Hayat Sungjin Cho Hyewhon Rhim Ambily Nath Indu Viswanath Ae Nim Pae Jae Yeol Lee Dong Joon Choo Hea-Young Park Choo |
| Institution: | 1. College of Pharmacy and Division of Life and Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea;2. Center for Neuroscience, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea;3. Center for Neuro-Medicine, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea;4. Department of Medicinal and Pharmaceutical Chemistry, School of Science, University of Science and Technology, 52 Eoeun Dong, Yuseong-Gu, Daejeon 305-333, Republic of Korea;5. Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea |
| Abstract: | 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. |
| Keywords: | 1-Amino-4-methylpiperazine Sulfonyl indole 3D QSAR Pharmacophore mapping |
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