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

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

Affiliation

  • 1 Discovery and Early Clinical Research, Sepracor Inc., 84 Waterford Drive, Marlborough, MA 01752, USA. liming.shao@sepracor.com
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.

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