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Start Over Author "Cho, Sungjin" Topic 3d qsar
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1. 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.

Author

Hayat, Faisal, Cho, Sungjin, Rhim, Hyewhon, Indu Viswanath, Ambily Nath, Pae, Ae Nim, Lee, Jae Yeol, Choo, Dong Joon, and Choo, Hea-Young Park

Subjects
*AMINO compounds, *PIPERAZINE, *BRAIN anatomy, *ANTIPSYCHOTIC agents, *ANTIDEPRESSANTS, *THERAPEUTICS, *CENTRAL nervous system diseases, *STRUCTURE-activity relationship in pharmacology
Abstract

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. [Copyright &y& Elsevier]

Published
2013
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