Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands
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-HT(1A) and serotonin re-uptake receptors which shows excellent pharmacokinetic parameters.
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.
LIGANDS FOR CARDIAC BETA1 ADRENOCEPTOR FOR IMAGING CONGESTIVE HEART FAILURE
Novel β1 adrenoreceptor ligands that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging) are provided. Methods of imaging, including methods of imaging congestive heart failure, are also provide
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Page/Page column 39
(2008/12/07)
Enantioselective parallel synthesis using polymer-supported chiral Co(salen) complexes
(matrix presented) The kinetic resolution of epoxides with phenols catalyzed by a polymer-supported Co(salen) complex is applied to the first enantioselective catalytic synthesis of parallel libraries. The corresponding 1-aryloxy-2-alcohols are obtained i
Peukert, Stefan,Jacobsen, Eric N.
p. 1245 - 1248
(2008/02/09)
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