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S1P receptor mediated activity of FTY720 phosphate mimics
Authors:Klemens Högenauer  Klaus Hinterding  Peter Nussbaumer
Institution:Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland
Abstract:Various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins were prepared as phosphate mimics of the chiral aminophosphate 1-P to act as agonists on the S1P1 receptor. It was found that amino phosphonates and amino carboxylates are potent S1P1 binders. β-Amino acid 11 could be shown to reversibly reduce blood lymphocyte counts in rats after po administration.
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