Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands

  • Bioorg Med Chem Lett. 1999 Nov 15;9(22):3243-8. doi: 10.1016/s0960-894x(99)00570-3.
M B van Niel  1 ,  M S Beer ,  J L Castro ,  S K Cheng ,  D C Evans ,  A Heald ,  L Hitzel ,  P Hunt ,  R Mortishire-Smith ,  D O'Connor ,  A P Watt ,  A M MacLeod
Affiliations
  • 1. Department of Chemistry, Merck, Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom. [email protected]
PMID: 10576696 DOI: 10.1016/s0960-894x(99)00570-3
Abstract

A solution phase synthesis for the preparation of 3-aryloxy-2-propanolamine libraries has been developed. This resulted in the identification of 5 as a ligand with dual affinity for 5-HT1A and serotonin reuptake receptors which shows excellent pharmacokinetic parameters.