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Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands
M B van Niel1, M S Beer, J L Castro
1Department of Chemistry, Merck, Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom. Monique_vanniel@merck.com
Bioorganic & Medicinal Chemistry Letters
|November 27, 1999
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.