Abstract
Arylpiperzine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated as novel antidepressant compounds. The various analogues were efficiently prepared and bio-assayed for binding to 5-HT(2A), 5-HT(2C) receptor, and 5-HT transporter. Based on their in vitro and in vivo activities as well as selectivity over other neurotransmitter receptors and PK profiles, 33 and 34 were identified as lead compounds. Consequently, this pyrrole series of compounds appears to be promising enough to warrant further investigation.
Copyright 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacokinetics
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Animals
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Antidepressive Agents / chemical synthesis
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Antidepressive Agents / chemistry*
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Antidepressive Agents / pharmacokinetics
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Injections, Intravenous
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Mice
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Piperazine
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacokinetics
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Pyrroles / chemical synthesis
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Pyrroles / chemistry*
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Pyrroles / pharmacokinetics
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Rats
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Receptor, Serotonin, 5-HT2A / metabolism
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Receptor, Serotonin, 5-HT2C / metabolism
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Selective Serotonin Reuptake Inhibitors / chemical synthesis
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Selective Serotonin Reuptake Inhibitors / chemistry*
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Selective Serotonin Reuptake Inhibitors / pharmacokinetics
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Serotonin 5-HT2 Receptor Antagonists*
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Serotonin Plasma Membrane Transport Proteins / chemistry*
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Serotonin Plasma Membrane Transport Proteins / metabolism
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Structure-Activity Relationship
Substances
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Amides
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Antidepressive Agents
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Piperazines
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Pyrroles
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Serotonin 5-HT2 Receptor Antagonists
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Serotonin Plasma Membrane Transport Proteins
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Serotonin Uptake Inhibitors
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Piperazine