1. Academic Validation
  2. S1P receptor mediated activity of FTY720 phosphate mimics

S1P receptor mediated activity of FTY720 phosphate mimics

  • Bioorg Med Chem Lett. 2010 Mar 1;20(5):1485-7. doi: 10.1016/j.bmcl.2010.01.118.
Klemens Högenauer 1 Klaus Hinterding Peter Nussbaumer
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland. klemens.hoegenauer@novartis.com
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 S1P(1) receptor. It was found that amino phosphonates and amino carboxylates are potent S1P(1) Binders. beta-Amino acid 11 could be shown to reversibly reduce blood lymphocyte counts in rats after po administration.

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