S1P receptor mediated activity of FTY720 phosphate mimics

This work describes various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins to act as agonists on the S1P 1 receptor. Various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins were prepared as phosphate mimics of...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1485-1487
Hauptverfasser: Högenauer, Klemens, Hinterding, Klaus, Nussbaumer, Peter
Format: Artikel
Sprache:eng
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Zusammenfassung:This work describes various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins to act as agonists on the S1P 1 receptor. 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. β-Amino acid 11 could be shown to reversibly reduce blood lymphocyte counts in rats after po administration.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.118