Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.

Chen Chen,Brian Dyck,Beth A Fleck,Alan C Foster,Jonathan Grey,Florence Jovic,Michael Mesleh,Kasey Phan,Junko Tamiya,Troy Vickers,Mingzhu Zhang

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

Derivatives of milnacipran were synthesized and studied as monoamine transporter inhibitors. Potent analogs were discovered at NET (9k) and at both NET and SERT (9s and 9u). A pharmacophore model was established based on the conformational analysis of milnacipran in aqueous solution using NMR techniques and was consistent with the SAR results.

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关键词

Structure–activity relationship,Pharmacophore,Milnacipran,Norepinephrine,Serotonin,Monoamine transporter,Inhibitor,Synthesis

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