Abstract
Herein, we report the synthesis of thioridazine-VLA-4 hybrid epimers. These hybrid molecules were obtained by means of a click reaction involving N-propargyl northioridazine enantiomers and an azide containing VLA-4 antagonist. A synthesis of northioridazine enantiomers from racemic thioridazine was developed and the absolute stereochemistry was confirmed by X-ray crystallography. Access to N-substituted thioridazine analogs may reveal that this phenothiazine core has therapeutic potential in other disease avenues.
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