Abstract
Novel azetidines based on the 3-aryl-3-oxypropylamine scaffold were designed, synthesized, and evaluated as TRIs. Reduction of 1 followed by Swern oxidation and then Grignard reaction gave 3. The alkylation of 3 provided the corresponding azetidine derivatives 6, of which the two most promising, 6bd and 6be, were selected from 86 prepared analogues based on their biological profiles. Compound 6be showed activity in vivo in FST at 10 mg/kg IV or 20-40 mg/kg PO.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Antidepressive Agents / pharmacology*
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Azetidines / chemical synthesis
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Azetidines / chemistry*
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Azetidines / pharmacokinetics
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Azetidines / pharmacology*
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Behavior, Animal / drug effects
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Drug Design*
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HEK293 Cells
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Humans
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Inhibitory Concentration 50
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Mice
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Neurotransmitter Uptake Inhibitors / chemical synthesis
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Neurotransmitter Uptake Inhibitors / chemistry*
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Neurotransmitter Uptake Inhibitors / pharmacokinetics
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Neurotransmitter Uptake Inhibitors / pharmacology*
Substances
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Antidepressive Agents
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Azetidines
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Neurotransmitter Uptake Inhibitors
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azetidine