Article ID Journal Published Year Pages File Type
1373926 Bioorganic & Medicinal Chemistry Letters 2009 6 Pages PDF
Abstract

Single enantiomer [(aryloxy)(pyridinyl)methyl]piperidine and pyrrolidine derivatives 5–9 are inhibitors of monoamine reuptake. Structure–activity relationships established that monoamine reuptake inhibition are functions of amine, pyridine isomer, aryloxy ring substitution and stereochemistry. Consequently, selective NRIs, selective SRIs, dual SNRIs and triple SNDRIs were all identified. Dual SNRIs 5l–a and 9c were evaluated in additional pharmacology and pharmacokinetic studies as representative examples from this series.

Graphical abstract[(Aryloxy)(pyridinyl)methyl]piperidine and pyrrolidine derivatives 5–9 are inhibitors of monoamine reuptake. Structure–activity relationships established that monoamine reuptake inhibition are functions of amine, pyridine isomer, aryloxy ring substitution and stereochemistry. Consequently, selective NRIs, selective SRIs, dual SNRIs and triple SNDRIs were all identified. Dual SNRIs 5l–a and 9c were evaluated in additional pharmacology and pharmacokinetic studies as representative examples from this series.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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