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

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

Affiliation

  • 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.

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