Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. doi: 10.1016/j.bmcl.2008.10.026.
Puwen Zhang  1 ,  Eugene A Terefenko ,  Casey C McComas ,  Paige E Mahaney ,  An Vu ,  Eugene Trybulski ,  Elizabeth Koury ,  Grace Johnston ,  Jenifer Bray ,  Darlene Deecher
Affiliations
  • 1. Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. [email protected]
PMID: 18951020 DOI: 10.1016/j.bmcl.2008.10.026
Abstract

A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxetine and atomoxetine (4 and 5).