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

…, P Hunt, R Mortishire-Smith, D O'Connor…

Index: Van Niel, Monique B.; Beer, Margaret S.; Castro, Jose L.; Cheng, Susan K.F.; Evans, David C.; Heald, Anne; Hitzel, Laure; Hunt, Peter; Mortishire-Smith, Russell; O'Connor, Desmond; Watt, Alan P.; MacLeod, Angus M. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 22 p. 3243 - 3248

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Citation Number: 16

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 re-uptake receptors which shows excellent pharmacokinetic parameters.