Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint

  • Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. doi: 10.1016/j.bmcl.2008.07.050.
Sarah Hudson  1 ,  Mehrak Kiankarimi ,  Wendy Eccles ,  Yalda S Mostofi ,  Marc J Genicot ,  Wesley Dwight ,  Beth A Fleck ,  Kathleen Gogas ,  Warren S Wade
Affiliations
  • 1. Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. [email protected]
PMID: 18667309 DOI: 10.1016/j.bmcl.2008.07.050
Abstract

The design, synthesis and SAR of a series of heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. As racemates, the best compounds compare favorably with atomoxetine (IC(50)'s<10 nM) in potency at the transporter.