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

M B van Niel; 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

doi:10.1016/s0960-894x(99)00570-3

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.

Authors

M B van Niel¹, 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

Affiliation

¹ Department of Chemistry, Merck, Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom. Monique_vanniel@merck.com

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.

MeSH terms

Ligands
Propanolamines / chemical synthesis*
Propanolamines / metabolism
Propanolamines / pharmacokinetics
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
Selective Serotonin Reuptake Inhibitors / metabolism
Selective Serotonin Reuptake Inhibitors / pharmacokinetics
Serotonin / metabolism*

Substances

Ligands
Propanolamines
Serotonin Uptake Inhibitors
Serotonin