2. Academic Validation
  3. Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint

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

Affiliation

  • 1 Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. shudson@neurocrine.com
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.

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