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

  • Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. doi: 10.1016/j.bmcl.2008.01.011.
Chen Chen  1 ,  Brian Dyck ,  Beth A Fleck ,  Alan C Foster ,  Jonathan Grey ,  Florence Jovic ,  Michael Mesleh ,  Kasey Phan ,  Junko Tamiya ,  Troy Vickers ,  Mingzhu Zhang
Affiliations
  • 1. Department of Medicinal Chemistry, Neurocrine Bioscience, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
PMID: 18207394 DOI: 10.1016/j.bmcl.2008.01.011
Abstract

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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