Discovery and structure-activity relationships of novel selective norepinephrine and dual serotonin/norepinephrine reuptake inhibitors |
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Authors: | Boot John Cases Manuel Clark Barry P Findlay Jeremy Gallagher Peter T Hayhurst Lorna Man Teresa Montalbetti Christian Rathmell Richard E Rudyk Hélène Walter Magnus W Whatton Maria Wood Virginia |
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Institution: | Eli Lilly and Co. Ltd, Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK. |
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Abstract: | Novel arylthiomethyl morpholines are potent selective norepinephrine reuptake inhibitors (NERIs) and dual serotonin/norepinephrine reuptake inhibitors (SRI/NERIs). The target compounds were prepared using a stereochemically versatile synthesis featuring an aldol condensation as the key step. One enantiomer of the 2-methoxy-substituted analogue was found to be a potent and selective norepinephrine reuptake inhibitor, whereas the opposite enantiomer was a potent dual serotonin/norepinephrine reuptake inhibitor. |
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