Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors

  • Bioorg Med Chem. 2011 Jan 1;19(1):663-76. doi: 10.1016/j.bmc.2010.10.034.
Liming Shao  1 ,  Fengjiang Wang ,  Scott C Malcolm ,  Jianguo Ma ,  Michael C Hewitt ,  Una C Campbell ,  Larry R Bush ,  Nancy A Spicer ,  Sharon R Engel ,  Lakshmi D Saraswat ,  Larry W Hardy ,  Patrick Koch ,  Rudy Schreiber ,  Kerry L Spear ,  Mark A Varney
Affiliations
  • 1. Discovery and Early Clinical Research, Sepracor Inc., 84 Waterford Drive, Marlborough, MA 01752, USA. [email protected]
PMID: 21093273 DOI: 10.1016/j.bmc.2010.10.034
Abstract

The present work describes a series of novel chiral amines that potently inhibit the in vitro reuptake of serotonin, norepinephrine and dopamine (triple reuptake inhibitors) and were active in vivo in a mouse model predictive of antidepressant like activity. The detailed synthesis and in vitro activity and ADME profile of compounds is described, which represent a previously undisclosed triple reuptake inhibitor chemotype.